Current research articles in the field of Medicinal Chemistry published in online journals.
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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:
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 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
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
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 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 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 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 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 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 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
Abstract The solvent extraction (SE) of garlic essential oil (Allium sativum) was studied. A multivariate study based on a four-factor, three-level Box–Behnken design (BBD) was used to evaluate the
influence of four major variables affecting the performance of the SE of garlic essential oil. The yield and the composition
of the essential oils from garlic obtained by SE were determined, and compared with those obtained by the supercritical fluid
extraction (SFE). Statistical treatment of the results provided by the BBD revealed that the selected parameters, extraction
time and extraction temperature, were significant. The essential oils were analyzed by gas chromatography–mass spectrometry
(GC–MS). Major essential oil components were 3-vinyl-4H-1,2-dithiin (31.89%), diallyl trisulfide (13.31%), diallyl sulfide
(2.22%), dially disulfide (6.87%), propyl allyl disulfide (13.89%), and dimethyl disulfide (7.05%). Compared with SFE, the
yield of essential oil obtained by SE was slightly lower, but major essential oil components were quantitatively similar.
Moreover, residual solvent in garlic essential oil was very low (<50 mg/kg). In addition, a significant increment in the ratio
of CD4+/CD8+ in serum of gastric cancer rats was determined after administration of garlic essential oil. It can be concluded, that the
SE method offers obvious advantages over SFE. Moreover, the results indicated that garlic essential oil may be useful for
treatment of patients with inflammatory disease, e.g., gastric cancer.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9255-z
Authors
Rui Li, The First Affiliated Hospital of Soochow University Department of Gastroenterology Suzhou China
Wei-chang Chen, The First Affiliated Hospital of Soochow University Department of Gastroenterology Suzhou China
Wei-peng Wang, Soochow University College of Pharmacy Suzhou 215007 China
Wen-yan Tian, The First Affiliated Hospital of Soochow University Department of Gastroenterology Suzhou China
Xue-guang Zhang, Key Laboratory of Medicine and Clinical Immunology of Jiangsu Province Suzhou 215006 China
Abstract A metabolomic method was established to investigate the plasma metabolic difference between healthy rabbits and rabbits with
Qi-stagnancy and blood stasis. All rabbits were administrated with an extraction of Salvia miltiorrhiza and S. miltiorrhiza coupled with Lignum dalbergiae odoriferae. The main compounds in plasma samples were detected by high-performance liquid chromatography/diode array detector/electrospray-mass
spectrometry (HPLC/DAD/ESI-MS). The data were analyzed by principal component analysis (PCA). The results showed that Qi-stagnancy
and blood stasis had a close relationship with dopamine. In addition, the results also indicated that the major plasma metabolic
difference between rabbits administrated with S. miltiorrhiza and S. miltiorrhiza coupled with Lignum dalbergiae odoriferae were 4-methylbenzamide, Danshensu and β-(3,4-dihydroxybenzene)-α-hydroxyl propanoic acid isopropyl ester. The above results could provide experimental evidence for the theory of traditional
Chinese medicine.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9275-8
Authors
Shi-Xiang Wang, Northwest University College of Life Sciences 195#, No. 229, Taibai North Road Xi’an 710069 China
Kai Luo, Northwest University Institute of Analytical Science/Shaanxi Provincial Key Laboratory of Electroanalytical Chemistry Xi’an 710069 China
Jing Liang, Northwest University Institute of Analytical Science/Shaanxi Provincial Key Laboratory of Electroanalytical Chemistry Xi’an 710069 China
Fei Fan, Northwest University College of Life Sciences 195#, No. 229, Taibai North Road Xi’an 710069 China
Hua Li, Northwest University Institute of Analytical Science/Shaanxi Provincial Key Laboratory of Electroanalytical Chemistry Xi’an 710069 China
Jian-Bin Zheng, Northwest University Institute of Analytical Science/Shaanxi Provincial Key Laboratory of Electroanalytical Chemistry Xi’an 710069 China
Xiao-Hui Zheng, Northwest University College of Life Sciences 195#, No. 229, Taibai North Road Xi’an 710069 China
Abstract Fexofenadine is a non-sedative and selective peripheral H1 receptor antagonist prescribed for allergic rhinitis and chronic urticaria. This article deals with a simple, feasible, and
sensitive isocratic reverse-phase high-performance liquid chromatographic method for the determination of fexofenadine hydrochloride
in bulk drug, pharmaceutical dosage forms and in human serum. The chromatography was carried out at 20 ± 2°C using two different
chromatographs and five different stationary phases. The isocratic mobile phase was phosphate buffer pH 7.4 and methanol (methanol–phosphate
buffer, 35:65, v/v), detection was made at 218 nm and the mobile phase flowed at 1 ml min−1. Validation parameters included linearity, accuracy, precision, specificity, limit of detection (LOD), limit of quantification
(LOQ), and robustness over a linearity range 5–15 μg ml−1 according to the ICH guidelines (r > 0.9999), the inter- and intra-day precisions were relative standard deviation (RSD) < 0.8%. The system suitability was
scrutinized by capacity factor, tailing factor, and number of theoretical plates (capacity factor > 2.0, tailing factor ≤ 2.0,
and theoretical plates > 2000). The retention time for five different stationary phases ranged from 3.78 to 4.15 min. The
LOD and LOQ for the procedure were executed on samples containing very low concentrations of analytes on two different commercial
brands of detectors.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9285-6
Authors
M. Saeed Arayne, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Najma Sultana, University of Karachi Department of Pharmaceutical Chemistry, Faculty of Pharmacy Karachi 75270 Pakistan
Hina Shehnaz, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Amir Haider, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Abstract The present research paper reports the synthesis and biological evaluation of 6-(3-substitutedpropoxyl)benzo[d][1,3]oxathiol-2-ones as potential atypical antipsychotic agents. Accordingly, 10 derivatives with either amino or aryloxy
substituents were synthesized. Potential antipsychotic activity of these compounds in terms of D2 antagonism was evaluated by their ability to inhibit apomorphine-induced climbing behavior in mice and 5-HT2 antagonistic activity of synthesized compounds was assessed by studying inhibition of 5-HTP-induced head twitches. Non-specific
D2 blockade was evaluated by studying propensity of these compounds to produce catalepsy in mice. All the synthesized compounds
were found to exhibit D2 and 5-HT2 antagonist activity in behavioral models. However, they also induced mild to severe catalepsy. Among the 10 compounds tested,
5b and 5e exhibited maximum ‘atypical antipsychotic activity like’ profile.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9278-5
Authors
Radha Charan Dash, Bharati Vidyapeeth University Department of Pharmaceutical Chemistry, Poona College of Pharmacy Pune 411038 India
Mugdha R. Suryawanshi, Bharati Vidyapeeth University Department of Pharmaceutical Chemistry, Poona College of Pharmacy Pune 411038 India
Suhas M. Shelke, Bharati Vidyapeeth University Department of Pharmaceutical Chemistry, Poona College of Pharmacy Pune 411038 India
Sharad H. Bhosale, Bharati Vidyapeeth University Department of Pharmaceutical Chemistry, Poona College of Pharmacy Pune 411038 India
Kakasaheb R. Mahadik, Bharati Vidyapeeth University Department of Pharmaceutical Chemistry, Poona College of Pharmacy Pune 411038 India
Abstract Haloperidol is a commonly used neuroleptic drug associated with a range of side effects. The aim of the study was to determine
in vitro interaction of haloperidol with human serum albumin (HSA) by 19F magnetic resonance spectroscopy (MRS) at 9.4 Tesla (T). The practical measurement based on fluorine resonance has been proposed
to determine drug level in HSA at 37°C.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9287-4
Authors
Dorota Bartusik, Institute for Biodiagnostics (West) National Research Council Canada 3330 Hospital Drive NW Calgary Alberta T2N 4N1 Canada
Boguslaw Tomanek, Institute for Biodiagnostics (West) National Research Council Canada 3330 Hospital Drive NW Calgary Alberta T2N 4N1 Canada
Barbara Blicharska, Jagiellonian University Institute of Physics Reymonta 4 30-059 Kraków Poland
Gino Fallone, Cross Cancer Institute Medical Physics Department 11560 University Ave Edmonton Alberta T6G 1Z2 Canada
Abstract In this study, a series of 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles (5a–t) were synthesized by condensing 4-amino-3-mercapto-(4H)-1,2,4-triazoles (4a–c) with different aromatic or aroyl acids through one-pot reaction. The compounds were evaluated for their anti-inflammatory,
analgesic, ulcerogenic, and lipid peroxidation actions. Some of the newly synthesized compounds showed very good anti-inflammatory
activity with low GI toxicity and reduced lipid peroxidation. These compounds also showed interesting profile of analgesic
activity in acetic acid-induced writhing test. The findings of the study indicate that the synthesized compounds have superior
GI safety profile along with reduction in lipid peroxidation as compared to that of the standard.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9281-x
Authors
Asif Husain, Jamia Hamdard University Department of Pharmaceutical Chemistry, Faculty of Pharmacy Hamdard Nagar New Delhi 110062 India
Md. Arif Naseer, Jamia Hamdard University Department of Pharmaceutical Chemistry, Faculty of Pharmacy Hamdard Nagar New Delhi 110062 India
Abstract Synthesis of a number of novel pregnane derivatives has been described in detail. They were prepared by reaction of 3β-hydroxy-5,
16-pregnadiene-20-one (2) with diethylene glycol, 2-methoxy ethanol, 1,2-propane diol, p-chloroaniline and p-fluoroaniline, respectively. The structures of these newly synthesized compounds have been established on basis of physical,
analytical and spectral data. These pregnane derivatives have been evaluated for their anti-dyslipidemic activity (Triton
model) and in vitro antioxidant activities. Out of the 12 compounds tested, 3 of them showed potent anti-dyslipidemic activity
and 7 showed potent antioxidant and scavenger of oxygen free radicals.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9280-y
Authors
Arun Sethi, University of Lucknow Department of Chemistry Lucknow 226007 India
Gitika Bhatia, Central Drug Research Institute Division of Biochemistry Lucknow 226001 India
Ashok K. Khanna, Central Drug Research Institute Division of Biochemistry Lucknow 226001 India
Mohammad Mobin Khan, Central Drug Research Institute Division of Biochemistry Lucknow 226001 India
Abha Bishnoi, University of Lucknow Department of Chemistry Lucknow 226007 India
Anil K. Pandey, University of Lucknow Department of Chemistry Lucknow 226007 India
Atul Maurya, University of Lucknow Department of Chemistry Lucknow 226007 India
Abstract The chemical composition of essential oil from magnolia collected in Suzhou city, China, was studied using gas chromatography-mass
spectroscopy. Fifty-four volatile compounds were identified in the essential oil, with eucalyptol (21.55%), β-Pinene(11.07%),
D-Limonene (8.93%), 1R-α-Pinene (7.86%), Bicyclo[2.2.1]heptan-2-one, 1,7,7-trimethyl-, (1R)-(6.46%), Cyclohexene, 4-methylene-1-(1-methylethyl)- (5.30%), 1,4-Cyclohexadiene, 1-methyl-4-(1-methylethyl)- (5.10%), camphene
(4.72%), being the major chemical constituents. In an in vivo approach, the protective effect of the essential oil against
oxidative stress in gastric cancer (GC) mice was also investigated in terms of superoxide dismutase, CAT, and glutathione
peroxidase activities. Our results indicate that the essential oil has an effective capability to enhance serum antioxidant
enzyme activities and sCD40L, and decrease phosphorylate-activate Akt protein levels in a dose-dependent manner in gastric
cencer mice. Overall, essential oil from magnolia appears to be an effective antioxidant and is quite suitable for further
biological evaluation.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9263-z
Authors
Rui Li, First Affiliated Hospital of Soochow University, Key Laboratory of Medicine and Clinical Immunology of Jiangsu Province Department of Gastroenterology Suzhou 215006 China
Wei-chang Chen, First Affiliated Hospital of Soochow University, Key Laboratory of Medicine and Clinical Immunology of Jiangsu Province Department of Gastroenterology Suzhou 215006 China
Wei-peng Wang, Soochow University College of Pharmacy Suzhou 215007 China
Wen-yan Tian, First Affiliated Hospital of Soochow University, Key Laboratory of Medicine and Clinical Immunology of Jiangsu Province Department of Gastroenterology Suzhou 215006 China
Xue-guang Zhang, Soochow University Institute of Medical Biotechnology Suzhou 215007 China
Abstract The essential oil from aerial parts of Psoralea pubescence (Miq.) Standl (Leguminoseae) was analyzed by gas chromatography (GC) and GC/mass spectroscopy systems. The major components
identified were psoralen (24.8%), bakuchiol (21.3%), β-caryophyllene (8.5%), germacrene D (6.8%), and α-humulene (4.6%). The
major volatiles released by β-glucosidase treatment of the aqueous plant residue were δ-pinene (28.3%), germacrene D (13.6%),
and tricyclene (10.2%). The oil showed significant antibacterial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, and Pseudomonas aeruginosa, while the β-glucosidase-liberated fraction was inactive.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9249-x
Authors
Hesham El-Seedi, Uppsala University Division of Pharmacognosy, Department of Medicinal Chemistry, Biomedical Centre Box 574 Uppsala 751 23 Sweden
Mervat Zayed, El-Menoufia University Department of Chemistry, Faculty of Science Shebin El-Kom 32512 Egypt
Shimaa Roshdy, El-Menoufia University Department of Chemistry, Faculty of Science Shebin El-Kom 32512 Egypt
Mohamed Salem, El-Menoufia University Genetic Engineering and Biotechnology Research Institute Shebin El-Kom 32512 Egypt
Mohamed Hawata, El-Menoufia University Department of Chemistry, Faculty of Science Shebin El-Kom 32512 Egypt
Farag El-Essawy, El-Menoufia University Department of Chemistry, Faculty of Science Shebin El-Kom 32512 Egypt
Mai El-Barbary, El-Menoufia University Department of Chemistry, Faculty of Science Shebin El-Kom 32512 Egypt
Salah El-Kousy, El-Menoufia University Department of Chemistry, Faculty of Science Shebin El-Kom 32512 Egypt
Abstract This study was designed to explore the antioxidant potential of hexane, chloroform, ethyl acetate, methanol, and water extract
of bark and leaves of Cassia siamea and Cassia javanica by superoxide anion radical scavenging assay. The different extracts showed significant inhibition of superoxide radicals
in a dose-dependant manner. Among all the bark extracts of C. siamea, the methanol extract showed the maximum inhibition of 60.5% at 800 μg/ml concentration and water extract also showed strong
antioxidant potential of 51.3% at 1000 μg/ml concentration. The water extract of bark of C. javanica showed strong antioxidant potential of 55% at 1000 μg/ml concentration. The various leaf extracts of C. siamea showed moderate antioxidant potential of 25–50% at 1000 μg/ml, whereas methanol leaf extract of C. javanica showed strong antioxidant potential of 50.4% at 300 μg/ml concentration. This preliminary study indicates the antioxidant
activity of the bark and leaves of C. siamea and C. javanica.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9274-9
Authors
Pawanjit Kaur, Guru Nanak Dev University Department of Botanical and Environmental Sciences Amritsar 143 005 Punjab India
Saroj Arora, Guru Nanak Dev University Department of Botanical and Environmental Sciences Amritsar 143 005 Punjab India
Abstract Simple spectrophotometric methods have been developed for the determination of six quinolone antibiotics, namely, ciprofloxacin,
gatifloxacin, norfloxacin, levofloxacin, ofloxacin, and pefloxacin, in pharmaceutical formulations using three different salts
of iron. These methods are based on the formation of complexes with ferric nitrate, ferric chloride, or iron ammonium citrate
in which the carboxylic group of quinolones undergoes complexation with iron. The complexes formed in these reactions, having
a brown color, were measured at their respective λmax values. The increase in absorbance was directly proportional to the concentration of quinolones and obeys Beer’s law in the
range of 6–300 μg mL−1 (r ≥ 0.9999). The proposed methods were optimized and validated per the guidelines of the International Conference on Harmonization.
The proposed methods were successfully employed for determination of these quinolones in pharmaceutical formulations.
Content Type Journal Article
Category Original Research
DOI 10.1007/s00044-009-9268-7
Authors
Farhan Ahmed Siddiqui, University of Karachi Department of Chemistry Karachi 75270 Pakistan
M. Saeed Arayne, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Najma Sultana, University of Karachi Research Institute of Pharmaceutical Sciences, Faculty of Pharmacy Karachi 75270 Pakistan
Agha Zeeshan Mirza, University of Karachi Department of Chemistry Karachi 75270 Pakistan
Faiza Qureshi, University of Karachi Department of Chemistry Karachi 75270 Pakistan
M. Hashim Zuberi, University of Karachi Department of Chemistry Karachi 75270 Pakistan
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