Current research articles in the field of Medicinal Chemistry published in online journals.
The author- or copyrights of the listed
research articles below
are held by the respective authors or site operators, who are also responsible
for the content of the presentations.
To search
this web page for specific words type "Ctrl" + "F" on your keyboard
(Command + "F" on a Mac). Then: type the word you are searching for in
the window that pops up!
To list your
article here plaease contact us by eMail.
On this page considered biochemistry journals:
Journal of Medicinal Chemistry - published by
The American Chemical Society, ACS -
As the most cited journal in Medicinal Chemistry, the Journal of Medicinal Chemistry focuses on original research dealing with chemical-biological relationships, mainly the bond between molecular structure and biological activity.
Enzyme Inhibition and Medicinal Chem - published by
Taylor & Francis -
... is an international and interdisciplinary vehicle publishing new knowledge and findings on enzyme inhibitors and inhibitory processes and agonist/antagonist receptor interactions in the development of medicinal and anti-cancer agents and an understanding of their action.
Medicinal Chemistry Research - published by
Springer -
... offers prompt publication of novel experimental achievements in the many facets of drug design, drug discovery, and the elucidation of mechanisms of action of biologically active compounds.
Current research articles of the mentioned
journals:
Two series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones were designed, synthesised, and evaluated
for their antibacterial activities and CDKs inhibitory activities. The pyridazine derivative: 6-phenyl-5-phenylhydrazono-2,3,4,5-tetrahydropyridazine-3,4-dione
(3a) revealed activity against Staphylococcus aureus as Gram-positive bacteria while compound 2-(2-Ethoxyphenyl-5-Phenylpiperazinosulfonamido)-3H-pyrido[2,3-d]pyrimidin-4-one (13c) was showing moderate antifungal activity against Candida albicans.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9328-z
Authors
Detlef Geffken, University of Hamburg Department of Pharmaceutical Chemistry, Institute of Pharmacy Hamburg Germany
Raafat Soliman, University of Alexandria Department of Pharmaceutical Chemistry, Faculty of Pharmacy Alexandria Egypt
Farid S. G. Soliman, University of Alexandria Department of Pharmaceutical Chemistry, Faculty of Pharmacy Alexandria Egypt
Magdi M. Abdel-Khalek, University of Alexandria Department of Pharmaceutical Chemistry, Faculty of Pharmacy Alexandria Egypt
Doaa A. E. Issa, University of Alexandria Department of Pharmaceutical Chemistry, Faculty of Pharmacy Alexandria Egypt
Modeling studies demonstrate that aryl piperazines (I), aryloxyalkylamines (II), phenylalkykamines (III) and indolylalkylamines (VI) may interact at 5-HT receptors in a similar manner. Examination of these structures (I–VI) reveals that all possess an aromatic moiety and terminal amine binding sites (Glennon et al., J Med Chem 32(8):1921–1926, 1989). In the present investigation a new series of aryloxyalkylamines (4, 5, 8, and 9) was designed and synthesized, in which the aromatic moiety is a phenyl group substituted at the 2,3-, 2,4-, 2,5-, or 2,6-positions
by halogens and the terminal amine is N-methylpiperazine, or morpholine. In addition, the alkyl side chain is ethyl, or substituted
ethyl at the α- or β-carbon by a methyl group. The length of the alkyl chain that separates the terminal amine from the ether
oxygen atom of the aryloxy group is of major importance, and two-carbon chain appears optimal. The structures of the new compounds
were assessed by microanalyses, IR, and NMR. The analgesic activity of selected compounds was performed on experimental animals
and proved to be in the range of 85–100% relative to aspirin.
Graphical Abstract
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9316-3
Authors
Abdulkhader M. Ismaiel, King Abdulaziz University Faculty of Pharmacy, Pharmaceutical Chemistry Department P. O. Box 80260 Jeddah 21589 Kingdom of Saudi Arabia
Laila M. Gad, King Abdulaziz University Faculty of Pharmacy, Pharmaceutical Chemistry Department P. O. Box 80260 Jeddah 21589 Kingdom of Saudi Arabia
Salah A. Ghareib, King Abdulaziz University Faculty of Pharmacy, Pharmacology and Toxicology Department P. O. Box 80260 Jeddah 21589 Kingdom of Saudi Arabia
Faida H. Bamanie, King Abdulaziz University Faculty of Faculty of medicine, Clinical Biochemistry Department P. O. Box 80260 Jeddah 21589 Kingdom of Saudi Arabia
Mohamed A. Moustafa, King Abdulaziz University Faculty of Pharmacy, Pharmaceutical Chemistry Department P. O. Box 80260 Jeddah 21589 Kingdom of Saudi Arabia
A series of Co(II), Ni(II), Cu(II), and Zn(II) complexes of Schiff base ligands L1H3 and L2H have been prepared. The ligands are synthesized by the condensation of 2-hydroxy-3-formylquinoline with salicyloylhydrazide
and 2-hydrazinobenzothiazole in absolute ethanol. The prepared complexes were characterized by the analytical and spectral
techniques. The stoichiometry of the complexes is found to be 1:1. The presence of coordinated and lattice water is confirmed
by the TG and DTA studies. Subsequently all the prepared complexes were screened for antimicrobial activity against bacteria
and fungi. The Cu(II) complexes have been found to be more active than the ligand. In addition the DNA binding/cleaving capacity
of the compounds was analyzed by absorption spectroscopy, viscosity measurement, thermal denaturation, and gel electrophoresis
methods.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9330-5
Authors
Gurunath S. Kurdekar, Karnatak University Department of Chemistry Pavate Nagar Dharwad 580 003 Karnataka India
Sathisha Mudigoudar Puttanagouda, Karnatak University Department of Chemistry Pavate Nagar Dharwad 580 003 Karnataka India
Naveen V. Kulkarni, Karnatak University Department of Chemistry Pavate Nagar Dharwad 580 003 Karnataka India
Srinivasa Budagumpi, Karnatak University Department of Chemistry Pavate Nagar Dharwad 580 003 Karnataka India
Vidyanand K. Revankar, Karnatak University Department of Chemistry Pavate Nagar Dharwad 580 003 Karnataka India
Non-nucleoside reverse transcriptase inhibitors (NNRTI) has a definitive role and most commonly used in treatment of HIV infection.
NNRTI act by binding to specific binding site (non-nucleoside binding pocket-NNBP) in reverse transcriptase (RT) enzyme. With
the objective of developing efficient NNRTI, we have designed various Isatin analogs for effective treatment of AIDS and were
subjected to molecular docking studies on five different crystal structures of RT complexed with five different ligands Nevirapine,
Delaviridine, Efavirenz, Etravirine, and Rilpivirine. Combined dock-score of compound N21, N11, N23 was found to be comparable
with standards indicated that Isatin analogs have good binding affinity for NNBP. Docking results suggested that these types
of compounds could be binding in the NNRTI binding site in a similar mode to a known non-nucleoside inhibitors. ADME properties
of Isatin analogs were also analyzed using Qikprop 2.5 tool of Schrodinger software.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9329-y
Authors
Vidya S. Pawar, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Deepak K. Lokwani, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Shashikant V. Bhandari, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Kailash G. Bothara, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Trupti S. Chitre, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Titiksh L. Devale, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Nileema S. Modhave, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Jignesh K. Parikh, AISSMS College of Pharmacy Department of Pharmaceutical Chemistry Near RTO, Kennedy Road Pune 411001 Maharashtra India
Eighteen 1,2,3,4-tetrahydro-2-thioxopyrimidine analogs (5a–j, 6a–e, and 7a–c) of combretastatin A-4 were synthesized with the objective of discovering compounds capable of controlling the growth of
Trypanosomalewisii, Leishmaniatarantole, Plasmodiumfalciparum, and Giardialamblia. Even though the target compounds demonstrated differential cytotoxicity against mammalian cancer cells, with IC50 values ranging from 0.5 to >100 μM, the range of activity against Trypanosoma, Leishmania, and Plasmodium, and to a good extent for Giardia, was narrow. The IC50 values of “active” compounds against the parasites ranged from about 10 μΜ to slightly greater than 50 μΜ. Specifically,
compounds 5a, 5g, 5h, 6c, 7a, and 7c were not cytotoxic against mammalian cancer cells (IC50 > 100 μM) but showed good activity against the parasites, except Giardia (e.g., compounds 6c and 7a), suggesting that these compounds may act in a similar mechanism in parasites. Compounds 5f and 6b were previously shown to promote microtubule depolymerization in mammalian cells.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9334-1
Authors
Dereje Desta, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Robert Sjoholm, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Lauren Lee, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Megan Lee, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Kristin Dittenhafer, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Sarah Canche, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Balaji Babu, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Sameer Chavda, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
Christie Dewar, Provincial Laboratory for Public Health 8440-112th Street Edmonton AB T6G 2J2 Canada
Stephanie Yanow, Provincial Laboratory for Public Health 8440-112th Street Edmonton AB T6G 2J2 Canada
Aaron A. Best, Hope College Department of Biology Holland MI 49422 USA
Moses Lee, Hope College Division of Natural and Applied Sciences, Department of Chemistry 35 E 12th Street Holland MI 49422 USA
This study deals with the quantitative structure-activity relationship (QSAR) study of a series of 5-alkylidenepyridazine-3
(2H)-one as a novel non cAMP-based antiplatelet agent, using molecular descriptor derived from the 3D representation of the model
with the CS Chem office version 8.0. Several types of molecular descriptor such as electronic, thermodynamic and steric have
been used to derive a QSAR model between platelet inhibitory activity and structural properties. The best model for the prediction
of platelet inhibitory activity was obtained by applying sequential multiple linear regression analysis method. Statically
significant model with r2 > 0.87 was obtained by using ovality (OV), dipole moment on z-axis (DPL3), HOMO energy (HE), standard Gibbs free energy (SGFE), total energy (TOE), torsion energy (TE) and non-1,4 VDW energy (NVDWE)
descriptors. Regression coefficient of all descriptors used is significant at more than 99% level. Result shows that dipole
moment DPL3 and OV are the principle descriptors for the inhibition of platelet aggregations. The model was also tested successfully
for internal q2 > 0.738 and external predictive r2 > 0.520 validation criteria. We demonstrate that the steric, topological and electronic descriptors play an important role
in inhibition of platelet aggregation of the alkylidenepyridazin-3-ones.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9333-2
Authors
Vivek K. Vays, Nirma University Department of Pharmaceutical Chemistry, Institute of Pharmacy S.G. Highway, Chharodi Ahmedabad 382 481 Gujarat India
Anurekha Jain, Rajiv Gandhi Technical University Department of Pharmaceutical Analysis, B. R. Nahata College of Pharmacy Mandasur 458 001 MP India
Manjunath Ghate, Nirma University Department of Pharmaceutical Chemistry, Institute of Pharmacy S.G. Highway, Chharodi Ahmedabad 382 481 Gujarat India
Deepika Maliwal, Rajiv Gandhi Technical University Department of Pharmaceutical Analysis, B. R. Nahata College of Pharmacy Mandasur 458 001 MP India
Dipeptidyl peptidase IV is a glycoprotein which removes N-terminal dipeptides from physiologically relevant polypeptides.
An homologous series of 6-imino-2-thioxo-5-{[3,4,5-tris(methyloxy)phenyl]methyl}-2,5-dihydro-4(3H)-pyrimidinones has been tested for inhibition of DPP IV activity. The inhibitory effects at 0.1 mM were observed. Enzyme
kinetic studies revealed that compounds inhibit DPP IV activity competitively. According to the molecular docking analysis,
the inhibitors are anchored into the DPP IV hydrolytic site by interactions of the pyrimidinone core with Glu206, Tyr662,
and Tyr547, with the alkyl chain entering the S1 pocket. We conclude that pyrimidinone-like compounds are a promising new
scaffold for reversible inhibition of DPP IV.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9314-5
Authors
Dubravko Jelić, GlaxoSmithKline Research Center Zagreb Ltd. Prilaz baruna Filipovića 29 10000 Zagreb Croatia
Krunoslav Nujić, GlaxoSmithKline Research Center Zagreb Ltd. Prilaz baruna Filipovića 29 10000 Zagreb Croatia
Višnja Stepanić, GlaxoSmithKline Research Center Zagreb Ltd. Prilaz baruna Filipovića 29 10000 Zagreb Croatia
Krunoslav Kovačević, GlaxoSmithKline Research Center Zagreb Ltd. Prilaz baruna Filipovića 29 10000 Zagreb Croatia
Donatella Verbanac, GlaxoSmithKline Research Center Zagreb Ltd. Prilaz baruna Filipovića 29 10000 Zagreb Croatia
The Co(II), Ni(II), and Cu(II) complexes with Schiff bases derived from 3-substituted-4-amino-5-mercapto-1,2,4-triazole and
fluvastatin have been synthesized. Schiff bases exhibited thiol–thione tautomerism and coordinated to metal ion through azomethine
nitrogen and thiolate sulphur atoms. Square planar geometry for all the metal complexes of the type ML2 has been proposed in the light of analytical, spectral (IR, UV–Vis., ESR, and FAB-mass), magnetic, and thermal studies. The
antimicrobial studies of Schiff bases and their metal complexes against various antibacterial (Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus subtilis) and antifungal (Aspergillus niger, and Pencillium Chrysogenum) species by Minimum Inhibitory Concentration method revealed that, the metal complexes possess more healing antibacterial
activity than the Schiff bases. Co(II), Ni(II), and Cu(II) complexes cleave the DNA isolated from A. niger.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9327-0
Authors
Ajaykumar D. Kulkarni, Karnatak University P.G. Department of Chemistry Dharwad 580003 Karnataka India
Sangamesh A. Patil, Karnatak University P.G. Department of Chemistry Dharwad 580003 Karnataka India
Vinod H. Naik, Karnatak University P.G. Department of Chemistry Dharwad 580003 Karnataka India
Prema S. Badami, Shri Sharanabasaveswar College of Science Department of Chemistry Gulbarga 585102 Karnataka India
A series of novel unsymmetrically disubstituted acylthioureas fused with hydrophenanthrene structure were synthesized from
Δ8-dihydroabietic and dehydroabietic acid, respectively. Their structures were characterized by IR, 1H-, and 13C-NMR spectroscopy. The antitumor activities of the title compounds against SMMC7721 and A549 tumor cells were evaluated by
MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The results showed that three compounds (4c1, 4d1, and 4d2) exhibited highly effective activities against SMMC7721 and A549 cells, their IC50 values are between 1.87–12.67 μM for SMMC7721 cells and 2.20–6.79 μM for A549 cells, respectively. Structure–activity relationship
indicating that acylthioureas that furan group fused with Δ8-dihydroabietyl group, trihydroxymethyl fused with Δ8-dihydroabietyl and dehydroabietyl could generate enhance activities of this kind of compounds against SMMC7721 and A549 cells.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9303-8
Authors
Xiao-Ping Rao, Chinese Academy of Forestry Institute of Chemical Industry of Forest Products Nanjing 210042 People’s Republic of China
Yong Wu, Chinese Academy of Forestry Institute of Chemical Industry of Forest Products Nanjing 210042 People’s Republic of China
Zhan-Qian Song, Chinese Academy of Forestry Institute of Chemical Industry of Forest Products Nanjing 210042 People’s Republic of China
Shi-Bin Shang, Chinese Academy of Forestry Institute of Chemical Industry of Forest Products Nanjing 210042 People’s Republic of China
Zong-De Wang, Chinese Academy of Forestry Institute of Chemical Industry of Forest Products Nanjing 210042 People’s Republic of China
The search for new antimalarial agents is necessary as current drugs in the market have become vulnerable due to the emergence
of resistant strains of Plasmodium falciparum (Pf). The enzyme dihydroorotatedehydrogenase (PfDHODH) is a validated target for development of antimalarial agents. PfDHODH is a crucial enzyme in the de novo pyrimidine biosynthesis pathway and is essential for the growth of the parasite.
In this article, we report the design, synthesis and evaluation of benzanilides as inhibitors of PfDHODH. From the pool of molecules designed using molecular modeling techniques, candidates were shortlisted for further evaluation
based on docking scores and 3D-QSAR studies. The activities of these shortlisted analogs were predicted from CoMFA and CoMSIA
models. The most promising molecules were synthesized using solvent-free microwave-assisted synthesis and their structures
characterized by spectroscopic techniques. The molecules were screened for in vitro antimalarial activity by the whole cell
assay method. Two molecules viz. KMC-3 and KMC-15 were found to be active at 8.7 and 5.7 μM concentrations, respectively.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9323-4
Authors
Kumar R. Desai, Bombay College of Pharmacy Department of Pharmaceutical Chemistry Kalina, Santacruz (E) Mumbai 400 098 India
Mushtaque S. Shaikh, Bombay College of Pharmacy Department of Pharmaceutical Chemistry Kalina, Santacruz (E) Mumbai 400 098 India
Evans C. Coutinho, Bombay College of Pharmacy Department of Pharmaceutical Chemistry Kalina, Santacruz (E) Mumbai 400 098 India
New anti-HIV-1 drugs that target different viral proteins or genes at various steps in the viral life cycle are highly expected.
HIV-1 assembly and disassembly (uncoating) processes are critical for the HIV-1 replication. HIV-1 capsid (CA) and human cyclophilin
A (CypA) play essential roles in these processes. Using an in vitro screening system, we evaluated 52 thiourea derivatives
for their potential CA and CypA-inhibiting activities. The antiviral activity of these compounds is correlated with their
CA assembly inhibitory ability and with their anti-PPIase activity, suggesting that these compounds could block HIV-1 replication
by disrupting CA assembly and inhibiting the PPIase activity of CypA to interfere with capsid disassembly. Among them, three
compounds D4, D5, and D6 displayed the most promising potency with CA-assembly rate 15.78, 18.42, and 7.97(×10−5) OD/s, and their IC50 for inhibition of PPIase activity 0.45, 0.65, and 0.33 μM, respectively. The potent protein inhibitory activity resulted
in their very low EC50 values (≤1.00 μM). They can be used for rational design of novel anti-HIV-1 drugs.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9315-4
Authors
Zhiwu Tan, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs NO. 38, Haidian District Beijing People’s Republic of China
Jiebo Li, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs NO. 38, Haidian District Beijing People’s Republic of China
Ruifang Pang, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs NO. 38, Haidian District Beijing People’s Republic of China
Shanshan He, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs NO. 38, Haidian District Beijing People’s Republic of China
Meizi He, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs NO. 38, Haidian District Beijing People’s Republic of China
Shixing Tang, Food and Drug Administration Center for Biologics Evaluation and Research Bethesda MD 20892 USA
Indira Hewlett, Food and Drug Administration Center for Biologics Evaluation and Research Bethesda MD 20892 USA
Ming Yang, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs NO. 38, Haidian District Beijing People’s Republic of China
The present study evaluated the hepatoprotective properties of Morinda pubescens fruit extract against d-galactosamine (d-GalN)-induced liver injury in rats. The fruit extract of M. pubescens was administrated orally at 200 mg/kg of body weight daily once for 21 days and at 21st day, d-GalN (500 mg/kg of body weight) was injected intraperitoneally in rats, to induce liver damage. In d-GalN administrated rats, significant increase in the levels of serum marker enzymes and lipid peroxidation (LPO) in liver
and decreased serum and liver antioxidant levels were observed. Pre-treatment with fruit extract to rats reduced the elevated
levels of serum marker enzymes and also improves the levels of fucose, ceruloplasmin, and uric acid. Administration of M. pubescens fruit extract prevented increase of LPO and alteration in iron content in experimental animals, besides, considerably increased
the levels of glutathione (GSH) and vitamin E when compared to d-GalN intoxicated animals. The present results suggest that the M. pubescens fruit extract has liver-protective property against d-GalN-induced liver injury in rats, which was further confirmed by histopathological studies. The hepatoprotective potentials
of fruits of M. pubescens may be due to the presence of phenols and alkaloids, as analyzed by preliminary phytochemical analysis of fruit extract.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9317-2
Authors
G. Surendiran, University of Madras Biocontrol and Microbial Metabolites Lab, Centre for Advanced Studies in Botany Guindy Campus Chennai 600 025 Tamil Nadu India
N. Mathivanan, University of Madras Biocontrol and Microbial Metabolites Lab, Centre for Advanced Studies in Botany Guindy Campus Chennai 600 025 Tamil Nadu India
A series of the novel pyrimidine (3–6) and purine (12–15, 18–21) acyclic nucleoside analogues in which the sugar moiety was replaced by a sterically constrained Z-4-amino-, 4-aminohydrochloride-2-butenyl, or aliphatic 4-aminohydrochloride-2-butyl moiety were synthesized and evaluated
for their anti-viral and cytostatic activity potency. Cytostatic evaluation of the novel compounds on selected panel of human
tumour-cell lines showed that the majority of compounds exerted a non-specific anti-proliferative effect at the highest tested
concentration (i.e. 1 × 10−4 M) against all cell lines. Nevertheless, a rather moderate but selective anti-proliferative effects on HeLa cell cultures
in comparison to normal fibroblasts WI 38, were observed for compounds 15 and 21. No anti-viral activity was observed, except for compounds 3, 4, 5 and 19 that showed anti-HIV activity at 50% effective concentration ranging between 10 and 96 μM.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9318-1
Authors
Karlo Wittine, University of Zagreb Department of Organic Chemistry, Faculty of Chemical Engineering and Technology Marulićev trg 19 10000 Zagreb Croatia
Krešimir Benci, University of Zagreb Department of Organic Chemistry, Faculty of Chemical Engineering and Technology Marulićev trg 19 10000 Zagreb Croatia
Sandra Kraljević Pavelić, Ruđer Bošković Institute Division of Molecular Medicine, Laboratory for systems biomedicine Bijenička cesta 54 P. O. Box 1016 10001 Zagreb Croatia
Krešimir Pavelić, Ruđer Bošković Institute Division of Molecular Medicine, Laboratory for systems biomedicine Bijenička cesta 54 P. O. Box 1016 10001 Zagreb Croatia
Siniša Bratulić, Ruđer Bošković Institute Division of Molecular Medicine, Laboratory for systems biomedicine Bijenička cesta 54 P. O. Box 1016 10001 Zagreb Croatia
Karlo Hock, Ruđer Bošković Institute Division of Molecular Medicine, Laboratory for systems biomedicine Bijenička cesta 54 P. O. Box 1016 10001 Zagreb Croatia
Jan Balzarini, Katholieke Universiteit Leuven Rega Institute for Medical Research Minderbroedersstraat 10 B-3000 Leuven Belgium
Mladen Mintas, University of Zagreb Department of Organic Chemistry, Faculty of Chemical Engineering and Technology Marulićev trg 19 10000 Zagreb Croatia
A series of new coumarin derivatives 4 containing a chalcone moiety were synthesized by condensation of 3-acetyl-4-hydroxycoumarin 1 with aryl or heteroaryl aldehydes 2 in the presence of piperidine in chloroform. The interaction of 3-formyl-4-chloro-coumarin 3 with nitrogen compound nucleophiles are described and lead to the corresponding substituted chromen[4,3-c] pyrazol-4-ones
5. The structures of the obtained compounds were established on the basis of IR|1D|2D NMR, while crystal structure of 3-acetyl-4-hydroxy
coumarin 1 was determined using X-ray diffraction and further were evaluated for possible antibacterial and antioxidant activities.
The coumarinic chalcone 4d has been found to be the most active (IC50 = 2.07 μM) in this study.
Content Type Journal Article
Category Review
DOI 10.1007/s00044-010-9326-1
Authors
Naceur Hamdi, Borj Cedria Higher Institute of Sciences and Technology Environment Touristic Road of Soliman B.P. 95. 2050 Hammam-Lif Tunisia
Cédric Fischmeister, Université Rennes 1, Laboratoire Catalyse et Organométalliques CNRS-UMR “Sciences Chimiques de Rennes” 263 avenue du général Leclerc Bâtiment 10C 35042 Rennes cedex France
M. Carmen Puerta, Universidad de Cádiz Departamento de Ciencia de los Materiales Ingeniería Metalúrgica y Química Inorgánica, Facultad de Ciencias Campus del Río San Pedro 11510 Puerto Real Spain
Pedro Valerga, Universidad de Cádiz Departamento de Ciencia de los Materiales Ingeniería Metalúrgica y Química Inorgánica, Facultad de Ciencias Campus del Río San Pedro 11510 Puerto Real Spain
A series of bisacridine-1,8-dione derivatives were synthesized by one-pot reaction of aromatic dialdehydes, dimedone or cyclohexane-1,3-dione
and primer aromatic amines in acetonitrile to utilizing Amberlyst-15 as a heterogeneous catalyst. The structures of compounds
were characterized by FT-IR, NMR, and elemental analysis. Antimicrobial activities of these compounds were determined by using
the disc diffusion method against to these gram-positive and gram-negative bacteria and yeast. The results were compared with
reference discs.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9321-6
Authors
Muharrem Kaya, Dumlupınar University Faculty of Science and Arts, Chemistry Department 43100 Kütahya Turkey
Yılmaz Yıldırır, Gazi University Faculty of Science and Arts, Chemistry Department Teknikokullar 06500 Ankara Turkey
Gökçen Y. Çelik, Niğde University Faculty of Science and Arts, Biology Department 51240 Niğde Turkey
Fourteen newly synthesized derivatives of indophenazine 1,3,5-trisubstituted pyrazoline bearing benzofuran were prepared from
benzofuran chalcones with indophenazine hydrazide through cycloaddition reaction. All the compounds were screened for their
in vitro and in vivo antitubercular activity against drug resistant and multidrug-resistant Mycobacterium tuberculosis H37RV. The MIC50 and MIC90 were estimated and compared with rifampicin and gatifloxacin standard drugs. Nitro group containing at ortho5j, meta5e, furan ring containing 5m and ortho5i, para5h chloro containing compounds were exhibited significant in vitro, in vivo antitubercular activity against standard drugs.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9322-5
Authors
Kuntal Manna, Nirma University Department of Pharmaceutical Chemistry, Institute of Pharmacy Sarkhej-Gandhinagar Highway Ahmedabad 382481 Gujarat India
Yadvendra K. Agrawal, Gujarat Forensic Sciences University Institute of Research and Development Sector 18-A, Near Police Bhavan Gandhinagar 382007 Gujarat India
A series of levosimendan analogues were designed and synthesized, employing the Friedel–Crafts reaction, hydrolysis, and cyclization
from the key intermediate compound R(−)-6-(4-aminophenyl)-5-methyl-4, 5-dihydro-3(2H)-pyridazinone, which was obtained from the starting material, acetanilide.
These compounds, except 1b, exhibited potent anti-congestive heart failure activities, especially the compounds 1e and 1k, which showed more effective action than levosimendan.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9319-0
Authors
Lisheng Wang, Guangxi University College of Chemistry and Chemical Engineering Nanning 530004 China
Hongxiang Zhou, Guangxi University College of Chemistry and Chemical Engineering Nanning 530004 China
Bin Yang, Guangxi University College of Chemistry and Chemical Engineering Nanning 530004 China
Zhigang Chen, Guangxi University College of Chemistry and Chemical Engineering Nanning 530004 China
Hua Yang, Guangxi University College of Chemistry and Chemical Engineering Nanning 530004 China
The salicylic acid oxidation has been explained by a mechanism involving single electron transfer oxidation and single hydrogen
transfer using quantum chemistry calculations at the B3LYP theory level, together with the 6-311G** basis set. These methods
were employed to obtain energy (E), ionization potential (IP), bond dissociation energies (BDE), and spin density distribution of the salicylic acid. The results
show no discrepant behaviors between electron and hydrogen transfer in the regioselective hydroxylation of salicylic acid
by cytochrome P-450. The unpaired electron remains localized on the O7 phenolic oxygen (0.26 and 0.38), C1 carbon atoms at the carbonyl group (0.12 and 0.28), C2 carbon atom at the hydroxyl group (0.15 and 0.00), C3 carbon atom at the hydroxyl group (0.22 and 0.30), and C5 carbon atom (0.40 and 0.41) for cation free radical and semiquinone form, respectively. Calculations of spin densities showed
that chemistry reactivity is more favored in the positions C5 > C3 > C1 to form salicylate derivatives. These results supported the salicylic acid as scavenger derivatives in the lipid peroxidation.
Furthermore, we suggest a conventional proton and secondary electron abstraction, and semiquinone form by [1,5] hydrogen shift
between phenol and carbonyl groups.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9320-7
Authors
R. Santos Borges, Universidade Federal do Pará Faculdade de Farmácia, Laboratório de Química Farmacêutica, Instituto de Ciências da Saúde Belém PA 66075-110 Brazil
A. P. Salgado Mendes, Universidade Federal do Pará Faculdade de Farmácia, Laboratório de Química Farmacêutica, Instituto de Ciências da Saúde Belém PA 66075-110 Brazil
B. H. Souza e Silva, Universidade Federal do Pará Faculdade de Farmácia, Laboratório de Química Farmacêutica, Instituto de Ciências da Saúde Belém PA 66075-110 Brazil
C. Nahum Alves, Universidade Federal do Pará Faculdade de Química, Laboratório de Planejamento e Desenvolvimento de Fármacos, Instituto de Ciências Exatas e Naturais Belém PA 66075-110 Brazil
J. L. Martins do Nascimento, Universidade Federal do Pará Faculdade de Biologia e Biomedicina, Laboratório de Neuroquímica Molecular e Celular, Instituto de Ciências Biológicas Belém PA 66075-110 Brazil
A variety of N′-(4-(substituted phenyl amino)-6-(pyridin-2-ylamino)-1,3,5-triazin-2-yl)isonicotinohydrazide, 7a–r were synthesized by using 2-aminopyridine, isonicotic acid hydrazide and cyanuric chloride, and the structures of these compounds
were confirmed by IR and NMR (1H and 13C) spectral analyses. Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9324-3
Authors
Jignesh Priyakant Raval, New Vallabh Vidyanagar Department of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences (ARIBAS) Gujarat 388121 India
Nilesh Hasmukhbhai Patel, New Vallabh Vidyanagar Department of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences (ARIBAS) Gujarat 388121 India
Hemul Vinubhai Patel, New Vallabh Vidyanagar Department of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences (ARIBAS) Gujarat 388121 India
Pradip Shantibhai Patel, New Vallabh Vidyanagar Department of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences (ARIBAS) Gujarat 388121 India
Abstract Various thiazole-substituted thiadiazole derivatives (7a–t) were designed and synthesized using substituted acetophenones and substituted anilines as starting materials. Thiazole and
thiadiazole moieties being anticonvulsants were clubbed together to get the titled compounds and their in vivo anticonvulsant
screening were performed by two most adopted seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole
(scPTZ). Three compounds 7i, 7l and 7n were found to be potent in both the screens with comparable ED50 and better TD50 values than some standard drugs. These compounds were also found to exert lesser toxic effects on liver.
Content Type Journal Article
Category Original Paper
DOI 10.1007/s00044-010-9313-6
Authors
Nadeem Siddiqui, Hamdard University Department of Pharmaceutical Chemistry, Faculty of Pharmacy Hamdard Nagar New Delhi 110062 India
Waquar Ahsan, Hamdard University Department of Pharmaceutical Chemistry, Faculty of Pharmacy Hamdard Nagar New Delhi 110062 India
Abstract This study was aimed at evaluating the free radical scavenging activity of methanol extract and fractions from the bark of
Schleichera oleosa (Lour.) Oken by employing various well-established in vitro systems such as 2,2′-diphenyl-1-picrylhydrazyl (DPPH), deoxyribose
degradation (non-site specific and site specific), reducing power, chelating power, and plasmid nicking assays. Total Phenol
Content of the extracts was determined by the assay based on Folin-Ciocalteu’s method. In all the assays, it was observed
that the residue fraction, left after the precipitation, was more effective in scavenging the free radicals than the aqueous
extract and precipitates. The higher activity of residue fraction may be attributed to the greater amount of phenolic content
present in it (942.4 mg/g GAE) as compared to precipitates and aqueous extract. The extract and fractions were found to possess
potent antiradical properties, which may be due to either direct scavenging of free radicals or through metal chelation.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9297-2
Authors
Tarunpreet Singh Thind, Guru Nanak Dev University Department of Botanical and Environmental Sciences Amritsar 143005 Punjab India
Rajbir Singh, Guru Nanak Dev University Department of Botanical and Environmental Sciences Amritsar 143005 Punjab India
Rajbir Kaur, Guru Nanak Dev University Department of Botanical and Environmental Sciences Amritsar 143005 Punjab India
Geetanjali Rampal, Guru Nanak Dev University Department of Botanical and Environmental Sciences Amritsar 143005 Punjab India
Saroj Arora, Guru Nanak Dev University Department of Botanical and Environmental Sciences Amritsar 143005 Punjab India
Abstract A new series of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives has been synthesized. The newly synthesized compounds were
characterized by analytical and spectral methods. Compounds were screened for central nervous system activity. Compounds 1, 5, 7, 10, 14 exhibited significant antidepressant, anxiolytic and anticonvulsant activity in comparison to the reference drugs.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9308-3
Authors
Rajesh Sharma, Devi Ahilya Vishwavidyalaya School of Pharmacy Thakshyasila Campus, Khandwa Road Indore Madhya Pradesh 452 001 India
Ganesh Prasad Misra, Devi Ahilya Vishwavidyalaya School of Pharmacy Thakshyasila Campus, Khandwa Road Indore Madhya Pradesh 452 001 India
Jitendra Sainy, Devi Ahilya Vishwavidyalaya School of Pharmacy Thakshyasila Campus, Khandwa Road Indore Madhya Pradesh 452 001 India
Subhash Chandra Chaturvedi, IPS Academy College of Pharmacy A.B. Road, Rau Indore Madhya Pradesh 452 001 India
Abstract Novel series of pyrazolo[3,4-b]pyridines with basic skeleton different from the known COX inhibitors were synthesized from 5-amino-1-[4-(aminosulfonyl)phenyl]-3-phenyl-1H-pyrazole, which in turn was prepared by the condensation of (4-sulfamoylphenyl)hydrazine with α-cyanoacetophenone. All the
newly synthesized compounds were tested for their in vivo anti-inflammatory activity by carrageenan-induced rat paw edema
assay. Some of the most potent compounds were evaluated in different COX and LOX assays. Some of the new compounds were found
to possess moderate anti-inflammatory activity.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9312-7
Authors
Pawan K. Sharma, Kurukshetra University Department of Chemistry Kurukshetra 136119 India
Karan Singh, Kurukshetra University Department of Chemistry Kurukshetra 136119 India
Surender Kumar, Kurukshetra University Department of Chemistry Kurukshetra 136119 India
Pawan Kumar, Kurukshetra University Department of Chemistry Kurukshetra 136119 India
S. N. Dhawan, Kurukshetra University Department of Chemistry Kurukshetra 136119 India
Sukhbir Lal, Kurukshetra University Institute of Pharmaceutical Sciences Kurukshetra 136119 India
Holger Ulbrich, Johannes Gutenberg-University of Mainz Institute of Pharmacy Staudingerweg 5 55099 Mainz Germany
Gerd Dannhardt, Johannes Gutenberg-University of Mainz Institute of Pharmacy Staudingerweg 5 55099 Mainz Germany
Abstract The chemical forces responsible for interaction of drug (HIV-1-NNRTI) with receptor (HIV-1-NNRTI-binding pocket) have been
studied by evaluating log P and SASA for the measurement of hydrophobic interaction; energy of protonation (ΔE) for the measurement of most favorable hydrogen bond acceptor site; bond length and bond strain for the measurement of strength
of hydrogen bond formed between drug and receptor; ΔEnm‡ = ∣En‡ − Em‡∣ for the measurement of polar interaction. The molecular modeling and geometry optimization of the compounds (drugs) and
receptor amino acids (Val, Met, and Tyr) have been done using MOPAC-2002 associated with CAChe software. Softness Calculator
has been used to evaluate effective atomic softness (En‡ and Em‡). The results indicate that there is strong and effective hydrophobic interaction between hydrophobic substituent at site-6
of the drug and Val-Y187 of the receptor; hydrophobic substituent at site-5 and Met-Y184. Similarly, hydrogen bonds are formed
between N-atom (site-6) of the drug and H-atom of the phenolic group of the Tyr-Y188; between phenolic group of the Tyr-181
and H-atom (site-1) of the drug. Polar interaction (charge transfer) occurs between –C=O/S (site-2) of the drug and –CONH–
of Asn-Y182-Tyr-Y183.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9298-1
Authors
Ahmad Khalid Raza Khan, Maharani Lal Kunwari Post Graduate College Department of Chemistry Balrampur U.P. India
Suhail Ahmad Khan, Maharani Lal Kunwari Post Graduate College Department of Chemistry Balrampur U.P. India
Mohiuddin Ansari, Maharani Lal Kunwari Post Graduate College Department of Chemistry Balrampur U.P. India
Abstract The dinuclear cobalt(II) complexes with ciprofloxacin and bidentate ligands were synthesized and characterized using infrared
spectra, electronic spectra, magnetic measurements, elemental analyses, thermal investigation, and mass spectroscopy. Here
in we tried to increase an antibacterial activity of ciprofloxacin drug due to formation of mixed-ligand complexes. Synthesized
compounds were found to be more potent compared to drugs, ligands, and metal salt against selective gram(+ve) and gram(−ve) organisms. Interaction of the complexes with nucleic acid (DNA) was investigated using spectroscopic technique, viscosity
measurement, and gel electrophoresis and it was found that the complexes bind to DNA via intercalative mode.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9310-9
Authors
Mohan Patel, Sardar Patel University Department of Chemistry Vallabh Vidyanagar 388 120 Gujarat India
Mehul Chhasatia, Sardar Patel University Department of Chemistry Vallabh Vidyanagar 388 120 Gujarat India
Bhupesh Bhatt, Sardar Patel University Department of Chemistry Vallabh Vidyanagar 388 120 Gujarat India
Abstract A series of novel ketoprofen derivatives 4a–j bearing both amide and carbamate functionalities were prepared using the benzotriazole method of carboxylic and hydroxy group
activation. Selective reduction of ketoprofen produced hydroxy derivative 2, which in the reaction with one or two moles of 1-benzotriazole carboxylic acid chloride (1) gave benzotriazole derivatives 3a and 3b, respectively. Compounds 3a and 3b with various amines afforded amidocarbamates 4a–j. Antioxidative screenings revealed that the prepared compounds 3b and 4a–j possess excellent lipid peroxidation inhibition at 0.1 mM concentration, higher than 95% for the derivatives bearing aromatic,
cycloalkyl or heterocyclic substituents. Two of the compounds, 3b and 4g, also show high soybean lipoxygenase inhibition activity (95 and 83.5%, respectively). On the other hand, the amidocarbamate
derivatives of ketoprofen show only weak reducing activity against 1,1-diphenyl-2-picrylhydrazyl radicals. No selective antiviral
effects were noted for the tested compounds against a broad variety of DNA and RNA viruses. Most compounds were endowed with
a moderate (IC50: 10–25 μM) cytostatic activity.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9309-2
Authors
Zrinka Rajić, University of Zagreb Department of Medicinal Chemistry, Faculty of Pharmacy and Biochemistry A. Kovačića 1 10000 Zagreb Croatia
Dimitra Hadjipavlou-Litina, Aristotles University of Thessaloniki School of Pharmacy 541 24 Thessaloniki Greece
Eleni Pontiki, Aristotles University of Thessaloniki School of Pharmacy 541 24 Thessaloniki Greece
Jan Balzarini, Katholieke Universiteit Leuven Rega Institute for Medical Research 3000 Leuven Belgium
Branka Zorc, University of Zagreb Department of Medicinal Chemistry, Faculty of Pharmacy and Biochemistry A. Kovačića 1 10000 Zagreb Croatia
Abstract In this study, we have modified 4-hydroxy-pyran-2-ones, especially introduced heteroatoms (S or O) into the substituents, and detected their interactions with the binding pockets of HIV-1 protease (PR). The results indicated
that the ethoxyl groups at C-2′ and C-5′ of the phenyl ring could enhance the affinities to the S1′ and S2′ pockets and improve the inhibitory activities. The most potent compound 10f with an IC50 of 3.5 nM in enzymatic assay also exhibited good antiviral activity at the cellular level; it exhibited an EC50 value of 2.9 μM in Simian immunodeficiency virus-infected CEM cells and suppressed the PR activity in 293T cells using western
blot analysis.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9307-4
Authors
Meizi He, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs No. 38, Haidian District Beijing People’s Republic of China
Ning Yang, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs No. 38, Haidian District Beijing People’s Republic of China
Chunlai Sun, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs No. 38, Haidian District Beijing People’s Republic of China
Xiaojian Yao, University of Manitoba Laboratory of Molecular Human Retrovirology, Department of Medical Microbiology 508-745 William Avenue Winnipeg MB R3E OJ9 Canada
Ming Yang, Peking University Health Science Center State Key Laboratory of Natural and Biomimetic Drugs No. 38, Haidian District Beijing People’s Republic of China
Abstract A series of chalcone analogues and some of their derivatives were synthesized and subjected to the mosquito larvicidal study.
Chalcones having electron releasing group(s) on either ring A or ring B showed high toxicity. Electron withdrawing group(s),
especially at ring B, reduced the activity of chalcones. The activity was abruptly decreased due to replacement of ring A
by CH3, extension of conjugation or blocking of α,β-unsaturated ketone part of chalcones by derivatization. Quantitative structure–activity
relationship (QSAR) studies of these compounds were performed using various spatial, electronic and physicochemical parameters.
Genetic Function approximation with linear and spline options was used as the chemometric tool for developing the QSAR models.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9305-6
Authors
Naznin A. Begum, Department of Chemistry, Siksha Bhavana, Visva Bharati Bio-Organic Chemistry Laboratory Santiniketan 731 235 West Bengal India
Nayan Roy, Department of Chemistry, Siksha Bhavana, Visva Bharati Bio-Organic Chemistry Laboratory Santiniketan 731 235 West Bengal India
Rajibul A. Laskar, Department of Chemistry, Siksha Bhavana, Visva Bharati Bio-Organic Chemistry Laboratory Santiniketan 731 235 West Bengal India
Kunal Roy, Jadavpur University Drug Theoretics and Cheminformatics Laboratory, Department of Pharmaceutical Technology Kolkata 700 032 India
Abstract This present study was undertaken to synthesize and investigate possible analgesic activities of some 2-(2-carboxyphenylsulfanyl)-N-(4-substitutedphenyl)acetamide derivatives that were designed by combining an analgesic drug thiosalicylic acid and the main
pharmacophore group of paracetamol, N-(4-substitutedphenylacetamide). Chemical structures of synthesized compounds were elucidated by IR, 1H-NMR, and Mass spectral data. Paracetamol, thiosalicylic acid and some of the synthesized compounds in the series exhibited
significant analgesic activities in hot-plate, tail-clip, and acetic acid-induced writhing tests. Compound 2d showed more potent analgesic activity than both paracetamol and thiosalicylic acid. None of the compounds changed the responses
of animals recorded in Rota-Rod or activity cage tests with respect to control values. Therefore, analgesic activities of
the synthesized compounds evaluated in this study were not caused by motor impairments or neurosedative effects.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9300-y
Authors
Ümide Demir Özkay, Anadolu University Faculty of Pharmacy, Department of Pharmacology 26470 Eskişehir Turkey
Yusuf Özkay, Anadolu University Faculty of Pharmacy, Department of Pharmaceutical Chemistry 26470 Eskişehir Turkey
Özgür Devrim Can, Anadolu University Faculty of Pharmacy, Department of Pharmacology 26470 Eskişehir Turkey
Abstract A new series of disulfonamides were synthesized and assayed as antimicrobial agents against Staphylococcus aureus, Bacillus cereus, and Escherichia coli. The quantitative structure–activity relationship analysis (QSAR) was applied to find out the correlation between experimentally
evaluated antimicrobial activities with various parameters of the compounds using stepwise multiple liner regression method.
The QSAR analysis revealed that the third-order average connectivity index
( 3 c\textA )
was found to have negative correlation. The best QSAR models were further validated by leave-one-out method of cross-validation.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9304-7
Authors
Saliha Alyar, Çankırı Karatekin University Department of Chemistry, Science and Art Faculty 18100 Çankırı Turkey
Neslihan Özbek, Ahi Evran University Department of Primary Education, Faculty of Education 40001 Kırşehir Turkey
Kübra Kuzukıran, Gazi University Department of Chemistry, Science and Art Faculty 06500 Ankara Turkey
Nurcan Karacan, Gazi University Department of Chemistry, Science and Art Faculty 06500 Ankara Turkey
Abstract Three dimensional quantitative structure activity relationship approach using CoMFA and CoMSIA was applied to a series of
4-quinolone derivatives as high-affinity ligands at the benzodiazepine site of brain GABAA receptors. For the purpose, 27 compounds were used to develop models. 3D-QSAR models with high-squared correlation coefficient of up
to 0.979 for CoMFA and 0.931 for CoMSIA were established. The robustness of the model was confirmed with the help of leave
one out cross-validation method with rcv2 values of up to 0.526 and 0.546 for CoMFA and CoMSIA, respectively. Developed models highlighted the importance of shape
of the molecules, i.e., steric descriptors for GABAA receptor binding.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9306-5
Authors
Anand Gaurav, Shobhit University School of Pharmaceutical Sciences Meerut 250110 India
Mange R. Yadav, The M.S University of Baroda Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan Vadodara 390001 India
Rajani Giridhar, The M.S University of Baroda Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan Vadodara 390001 India
Vertika Gautam, Shobhit University School of Pharmaceutical Sciences Meerut 250110 India
Ranjit Singh, Shobhit University School of Pharmaceutical Sciences Meerut 250110 India
Abstract Quantitative structure activity relationship analysis has been performed with 32 synthetically derived analogues for their
inhibitory effects on monoamine oxidase-A using two-dimensional topological descriptors. The topological descriptors used
being total structure connectivity index, mean square distance index, mean wiener index, all-path wiener index, kier flexibility
index, eccentric index and superpendentic index. The statistical analysis has shown that excellent results are obtained by
using multiple linear regression method. The best model was selected based on the highest R2 value (0.904). The results are discussed critically using variety of statistical parameters such as squared correlation coefficient
(R2), adjusted R2, predicted residual sum of square (PRESS) and Pogliani’s quality factor (Q). The models were validated by using the method of leave-one and leave-many out cross-validation methods.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9302-9
Authors
Vipin Kumar, Kurukshetra University Institute of Pharmaceutical Sciences Kurukshetra Haryana India 136119
Himangini Bansal, Kurukshetra University Institute of Pharmaceutical Sciences Kurukshetra Haryana India 136119
Abstract Three-dimensional quantitative structure activity relationship (3D-QSAR) models was developed using molecular field analysis
(MFA) for 36 anilinoquinazoline derivatives, inhibiting c-Src kinase. The QSAR model was developed using 29 compounds and
its predictive ability was assessed using a test set of seven compounds. The predictive 3D-QSAR model has conventional r2 values of 0.961 while the cross-validated coefficient q2 and bootstrap correlation coefficient rBS2 values of 0.910 and 0.957, respectively. The developed model provides a powerful tool to design potent c-Src inhibitors as
novel antitumor agents. Six new inhibitors were designed and their pIC50 were predicted.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9301-x
Authors
Pratigya Silakari, Dr. H. S. Gour University Department of Chemistry Sagar MP 470 003 India
Savitri Devi Srivastava, Dr. H. S. Gour University Department of Chemistry Sagar MP 470 003 India
Dharam Veer Kohli, Dr. H. S. Gour University Department of Pharmaceutical Sciences Sagar MP 470 003 India
Santosh Kumar Srivastava, Dr. H. S. Gour University Department of Chemistry Sagar MP 470 003 India
Gyati Silakari, Dr. H. S. Gour University Department of Pharmaceutical Sciences Sagar MP 470 003 India
Bhawna Vyas, Multani Mal modi College Department of Pharmaceutical Chemistry Patiala India
Om Silakari, Punjabi University Department of Pharmaceutical Sciences and Drug Research Patiala Punjab 147002 India
Abstract We have synthesized a series of novel isoxazolines via 1,3-dipolar cycloaddition of in situ generated nitrile oxide from 2,4-dimethoxy
benzaldoxime and naphthaldehyde oxime with 4-allyl-2-methoxyphenol derivatives. The synthesized compounds were evaluated for
anti-stress activity in acute stress (AS) induced peripheral changes. Adult male Sprague–Dawley rats, subjected to AS, cause
a significant increase in gastric ulceration, adrenal gland weight, plasma glucose, corticosterone levels, and creatine kinase
activity. Compounds 3d, 3g, 5b, 5c, 5d, and 5g displayed most promising anti-stress effect by reverting these peripheral stress parameters at a dose of 40 mg/kg p.o.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9299-0
Authors
Rakesh Maurya, Central Drug Research Institute, CSIR Division of Medicinal and Process Chemistry Lucknow 226 001 India
Ausaf Ahmad, Central Drug Research Institute, CSIR Division of Pharmacology Lucknow 226 001 India
Prasoon Gupta, Central Drug Research Institute, CSIR Division of Medicinal and Process Chemistry Lucknow 226 001 India
Kailash Chand, Central Drug Research Institute, CSIR Division of Medicinal and Process Chemistry Lucknow 226 001 India
Manmeet Kumar, Central Drug Research Institute, CSIR Division of Medicinal and Process Chemistry Lucknow 226 001 India
Jayendra, Central Drug Research Institute, CSIR Division of Medicinal and Process Chemistry Lucknow 226 001 India
Preeti Rawat, Central Drug Research Institute, CSIR Division of Medicinal and Process Chemistry Lucknow 226 001 India
Naila Rasheed, Central Drug Research Institute, CSIR Division of Pharmacology Lucknow 226 001 India
Gautam Palit, Central Drug Research Institute, CSIR Division of Pharmacology Lucknow 226 001 India
Abstract A new possible resource of antimicrobial and antineoplastic was discovered for the first time from the aerial part of Atractylodes macrocephala Koidz. which was commonly disposed as waste. A comparative analysis of the constituents from the petroleum ether extracts
of the aerial part and the rhizome of A. macrocephala was investigated by gas chromatography–mass spectrometry (GC/MS). Total of 21 compounds of the aerial part and 31 compounds
of the rhizome of A. macrocephala were determined. Although the extracts of the aerial part and the rhizome showed little chemical composition correlation,
both of them demonstrated antimicrobial and antitumor activities. Furthermore, the aerial part showed better cytotoxic activities
than the rhizome with CEM cell line of IC50 values being below 10 μg/ml. These results could indicate that fatty oils from the aerial part of A. macrocephala had great potential to be used as a source for natural medicines or health products.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-010-9311-8
Authors
Wei Peng, Second Military Medical University School of Pharmacy 325 Guohe Rd Shanghai 200433 China
Ting Han, Second Military Medical University School of Pharmacy 325 Guohe Rd Shanghai 200433 China
Wen-Bo Xin, Second Military Medical University School of Pharmacy 325 Guohe Rd Shanghai 200433 China
Xiao-Gang Zhang, Second Military Medical University School of Pharmacy 325 Guohe Rd Shanghai 200433 China
Qiao-Yan Zhang, Second Military Medical University School of Pharmacy 325 Guohe Rd Shanghai 200433 China
Min Jia, Second Military Medical University School of Pharmacy 325 Guohe Rd Shanghai 200433 China
Lu-Ping Qin, Second Military Medical University School of Pharmacy 325 Guohe Rd Shanghai 200433 China
Abstract A series of 8-methyl-2-substituted-3,6-dihydroimidazo[4,5-c]pyrazolo[3,4-e]pyridazine compounds have been synthesized in the present investigation utilizing Philips condensation (Philips, J Chem Soc
2393–2399, 1928). The anti-inflammatory activity of the synthesized compounds was evaluated using a carrageenin rat model.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9290-9
Authors
Ashish Kumar Tewari, Banaras Hindu University Department of Chemistry, Faculty of Science Varanasi India
Rashmi Dubey, Lucknow University Department of Chemistry Lucknow India
Anil Mishra, Lucknow University Department of Chemistry Lucknow India
Abstract Development and validation of an analytical spectral calibration method to quantify buclizine hydrochloride, which is a piperazine
derivative and used as a single active principle in pharmaceutical forms were done. The quantification of buclizine hydrochloride
was performed in the wavelength range of 218–226 nm at N = 6. The linear regression equation has been constructed using relationship between concentration and absorbance at 218,
220, 222, 224, and 226 nm. The developed method was applied directly and easily to the analysis of the pharmaceutical tablet
preparations. Mean %RSD was found to be 0.6231% (Longifene® tablet 25 mg). The method was completely validated and proven to be rugged. This validated UV spectrophotometric method is
potentially useful for a routine laboratory analysis because of its simplicity, rapidity, sensitivity, precision, and accuracy.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9286-5
Authors
Farhan Ahmed Siddiqui, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Agha Zeeshan Mirza, University of Karachi Department of Chemistry Karachi 75270 Pakistan
M. Hashim Zuberi, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Faiza Qureshi, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Abstract Employing basic principles of solution phase combinatorial chemistry, a solution phase combinatorial synthesis and screening
of mini libraries of 1,2,4-triazole derivatives has been carried out. 6 × 6 indexed mini libraries were synthesized comprising
of 36 compounds. The libraries were analyzed by liquid chromatography–mass spectrometry–mass spectrometry (LC–MS–MS) analysis.
All the synthesized mini libraries were screened for antifungal activity and by deconvolution methodology leads for every
fungi used for study were identified. The leads were synthesized individually and screened for activity. The antifungal activity
of individually synthesized leads was improved as anticipated, in comparison with that of any of the mini libraries.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9283-8
Authors
Manish Sudesh Bhatia, Bharati Vidyapeeth College of Pharmacy Department of Pharmaceutical Chemistry Near Chitranagri Kolhapur 416013 Maharashtra India
Bandu Eknath Zarekar, Bharati Vidyapeeth College of Pharmacy Department of Pharmaceutical Chemistry Near Chitranagri Kolhapur 416013 Maharashtra India
Prafulla Balkrishna Choudhari, Bharati Vidyapeeth College of Pharmacy Department of Pharmaceutical Chemistry Near Chitranagri Kolhapur 416013 Maharashtra India
Kundan Bhanudas Ingale, Bharati Vidyapeeth College of Pharmacy Department of Pharmaceutical Chemistry Near Chitranagri Kolhapur 416013 Maharashtra India
Neela Manish Bhatia, Bharati Vidyapeeth College of Pharmacy Department of Pharmaceutical Chemistry Near Chitranagri Kolhapur 416013 Maharashtra India
Abstract A series of thiophenol adducts (3a–m) were prepared by addition of thiophenol to chalcones (1a–m) in the presence of a catalytic amount of KOt-Bu in solvent free conditions. In addition, the antibacterial and antifungal in vitro properties were tested against some
human pathogenic microorganisms by employing the disk diffusion technique. A majority of compounds were remarkably active
against several of the microorganisms. Compound 3i was determined to be the most active compound.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9279-4
Authors
Mustafa Ceylan, Gaziosmanpasa University Department of Chemistry, Faculty of Arts and Sciences 60110 Tokat Turkey
Meliha Burcu Gürdere, Gaziosmanpasa University Department of Chemistry, Faculty of Arts and Sciences 60110 Tokat Turkey
İsa Karaman, Gaziosmanpasa University Department of Biology, Faculty of Arts and Sciences 60250 Tokat Turkey
Hayreddin Gezegen, Gaziosmanpasa University Department of Chemistry, Faculty of Arts and Sciences 60110 Tokat Turkey
Abstract A series of 3-chloro-1-(5H-dibenz[b,f]azepine-5yl)propan-1-one derivatives (2a–k) bearing different amino acids were synthesized by base condensation reaction. 3-Chloro-1-(5H-dibenz[b,f]azepine-5yl)propan-1-one(2) was obtained by N-acylation of 5H-dibenz[b,f]azepine (1). All the synthesized compounds were evaluated for their potential over antioxidant activities against inhibition of lipid
peroxidation by β-carotene and linoleic acid assay and inhibition of human low-density lipoprotein (LDL) oxidation assay.
Typically, compound 2 showed weak antioxidant activity, whereas coupling of different amino acids enhances the antioxidant activities based on
the presence of different functional groups. Among the derivatives, compound 2d showed significant antioxidant activities followed by 2h, 2i, 2j and 2k.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9292-7
Authors
H. Vijay Kumar, University of Mysore Department of Studies in Chemistry Manasagangotri Mysore Karnataka 570 006 India
C. Kishor Kumar, University of Mysore Department of Studies in Chemistry Manasagangotri Mysore Karnataka 570 006 India
Nagaraja Naik, University of Mysore Department of Studies in Chemistry Manasagangotri Mysore Karnataka 570 006 India
Abstract New benzo[b][1,4]thiazin-3(4H)-one derivatives (compounds 12a–p) were synthesized via Smiles rearrangement and assayed in vitro for their antimicrobial activity against Gram-positive, Gram-negative
bacteria and fungi. The antimicrobial activity of the benzo[b][1,4]thiazin-3(4H)-ones showed, on the whole, potent toward all tested Gram-positive and Gram-negative microorganism (minimal inhibitory concentration
ranging from 16 to 64 μg/ml), whereas weak effectiveness was exhibited against fungi. Data obtained suggested that 12g, 12i, and 12o exerted the best antibacterial activity against Gram-positive bacteria and compound 12b demonstrated the best inhibition of Gram-negative bacteria. These observations provide some predictions to design further
antimicrobial active compounds prior to their synthesis following with molecular modeling studies.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9288-3
Authors
Hao Yang, Southwest University College of Horticulture and Landscape Architecture 400715 Chongqing China
Liang Fang, The Ninth People’s Hospital of Chongqing Department of Oncology 400700 Chongqing China
Zhu-Bo Li, Southwest University College of Pharmaceutical Sciences 400715 Chongqing China
Fang-Kui Ren, Southwest University College of Pharmaceutical Sciences 400715 Chongqing China
Li-Ying Wang, Southwest University College of Pharmaceutical Sciences 400715 Chongqing China
Xiao Tian, Southwest University College of Pharmaceutical Sciences 400715 Chongqing China
Dong-Soo Shin, Changwon National University Department of Chemistry 641-773 Changwon South Korea
Hua Zuo, Southwest University College of Pharmaceutical Sciences 400715 Chongqing China
Abstract In the present study, we have synthesized chalcone and semicarbazide-linked chalonyl derivatives and the titled compounds
confirmed by MS, IR, and 1H NMR techniques. The anticonvulsant activity was determined by maximal electroshock (MES) induced seizure method. A majority
of the compounds exhibited significant anticonvulsant activity after intraperitoneal administration. The results show the
importance of hydrogen bonding for activity. In the present study 5e, 5h, 5i, 6e, 6h, and 6i emerged as the most active molecules, showed significant anticonvulsant of activity.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9277-6
Authors
Hemendra Pratap Singh, B N College of Pharmacy Udaipur Rajasthan India
S. N. Pandeya, Saroj Institute of Pharmacy Lucknow UP India
C. S. Chauhan, B N College of Pharmacy Udaipur Rajasthan India
Chandra Shekhar Sharma, B N College of Pharmacy Udaipur Rajasthan India
Abstract A series of novel indan-2-one and dibenzylidenepiperidin-4-one compounds were synthesized and screened for anticancer activities.
The compounds are symmetrical and they have conjugated double bonds. They closely resemble the curcumin analogs which are
found to possess anticancer properties. The structure of the compounds was confirmed by single crystal study and wherever
the compound is a powder, the structures were confirmed by spectral data (IR, NMR, and Mass).
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9284-7
Authors
Natesan Sundarmurthy Karthikeyan, VIT University Chemistry Division, School of Advanced Sciences Vellore 632 014 India
Kulathu Iyer Sathiyanarayanan, VIT University Chemistry Division, School of Advanced Sciences Vellore 632 014 India
Paduthapillai Gopal Aravindan, VIT University Physics Division, School of Advanced Sciences Vellore 632 014 India
P. Giridharan, Piramal Life Sciences Ltd. Mumbai 400 063 India
Abstract Twelve as yet, unreported complexes of luteolin were synthesized with various rare earth ions through refluxing in ethanol.
The characterization of these complexes by elemental analysis, infrared spectra, and differential scanning calorimeter demonstrated
that luteolin coordinated the various rare earth ions in a similar manner. Experiments designed to study the anti-inflammatory
activities of these rare earth-luteolin complexes indicated that they had a significant inhibitory effect on xylene-induced
ear edema in mice. Five complexes containing La3+, Ho3+, Yb3+, Lu3+, and Y3+ were equally effective as luteolin and dexamethasone (DXM). However, their inhibitory effects on carrageenan-induced paw
edema in mice, although significant, were weaker than that of either luteolin alone or DXM.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9289-2
Authors
Jingfen Li, Huzhou Teachers’ College Department of Life Science 313000 Huzhou China
Lisheng Wang, Guangxi University College of Chemistry and Chemical Engineering 530004 Nanning China
Haiqiang Bai, Guangxi University College of Chemistry and Chemical Engineering 530004 Nanning China
Bin Yang, Guangxi University College of Chemistry and Chemical Engineering 530004 Nanning China
Hua Yang, Guangxi University College of Chemistry and Chemical Engineering 530004 Nanning China
Abstract In order to construct a controlled release system of drugs and to reduce toxic side effects of 5-fluorouracil (5-FU), the
novel ramose chitosan-based-5-fluorouracil (CSFU) was synthesized by a two-step method. First, ramose N,N-dicarboxyethyl chitosan (CECS) was efficiently synthesized from chitosan (CS) through microwave irradiation under mild alkaline
media. Second, under the catalysis of EDC/NHS and using 5-Fu as a model drug, 1,3-bis(hydroxymethyl)-5-fluorouracil (HMFU)
was successfully linked to the ramose CECS. CSFU was characterized by IR spectrum, Raman Spectrum, and UV spectrum. The influence
of microwave irradiation time on degree of substitution (DS) of CECS was studied. The content of 5-FU in CSFU and its in vitro
release capability in phosphate buffer solution (PBS) were determined by UV spectrum. Results showed the drug loading (DL)
was 10.6% and its zero-order release time could sustain 42 h almost without burst release, which indicated its promising application
as a potential prodrug in cancer treatment.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9291-8
Authors
He-Ping Li, Changsha University of Science and Technology College of Chemical and Biologic Engineering Changsha 410004 China
Zhou-dong Wang, Changsha University of Science and Technology College of Chemical and Biologic Engineering Changsha 410004 China
Tao Yu, Changsha University of Science and Technology College of Chemical and Biologic Engineering Changsha 410004 China
Abstract Wound healing is a highly orchestrated process including complex and coordinated interactions involving peptide growth factors
of which transforming growth factor-beta (TGF-beta) is one of the most important modulators. Exogenous TGF-beta treatment
has been shown to accelerate wound healing in normal and impaired animal models. Nitric oxide (NO) also plays a key role in
wound healing. The objective of this study is to examine the effects of exogenous TGF-beta 1 treatment on NO and lipid peroxidation
levels in the process of oral wound healing on different days. In this study, we used 5-month-old New Zealand albino male
rabbits. After a standard surgical incision in the diestema region, the rabbits were divided into controls and TGF-beta 1
implanted groups. NO levels and malondialdeyhde (MDA) levels which are indicators of lipid peroxidation were determined by
spectrophotometry. In the TGF-beta 1 implanted groups, both NO and MDA levels significantly increased only on the third day
after wounding when compared to control groups. We found decreased MDA levels parallel to NO levels on the fifth day after
wounding. These findings suggest that TGF-beta 1 affects mucosal wound healing by altering NO production on different days
of wounding. TGF-beta 1 may regulate NO production by its dual effect in as both an activator and inhibitor an in oral mucosal
healing.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9276-7
Authors
Şule Coşkun, Gazi University Biology Department, Science and Arts Faculty 06500 Beşevler, Ankara Turkey
Emine Gülçeri Güleç Peker, Gazi University Biology Department, Science and Arts Faculty 06500 Beşevler, Ankara Turkey
Barbaros Balabanlı, Gazi University Biology Department, Science and Arts Faculty 06500 Beşevler, Ankara Turkey
Seyhan Ahıska, Ankara University Biology Department, Science Faculty 06500 Tandoğan, Ankara Turkey
Füsun Acartürk, Gazi University Department of Pharmaceutical Technology, Faculty of Pharmacy 06500 Etiler, Ankara Turkey
The author- or copyrights of the listed Internet pages
are held by the respective authors or site operators, who are also responsible
for the content of the presentations.
To add your company or product site to this index please use the
registration form or send us a eMail.
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 1917-1922, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2299-2308, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2146-2154, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2094-2103, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 1990-1999, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2314-2318, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 1951-1963, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2277-2285, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2319-2323, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2000-2009, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2051-2062, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2286-2298, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 1923-1936, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2171-2187, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2136-2145, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2063-2075, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2215-2226, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2126-2135, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2204-2214, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2324-2328, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 1964-1978, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2038-2050, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2155-2170, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 1979-1989, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2076-2086, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2239-2249, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2264-2276, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2227-2238, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2188-2196, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2250-2263, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2104-2113, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2309-2313, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2114-2125, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 1937-1950, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2087-2093, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2010-2037, March 11, 2010.
Journal of Medicinal Chemistry, Volume 53, Issue 5, Page 2197-2203, March 11, 2010.
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).
Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).