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Pharmaceutical Chemistry: Current Research Articles


 
Current Articles in the field of Pharmaceutical Chemistry published online in scientific 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.

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On this page considered biochemistry journals:


Pharmaceutical Chemistry Journal - published by Springer -
... is devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates.

Archiv der Pharmazie, Chemistry in Life Sciences - published by Wiley-Interscience -
... is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry.



Current research articles of the mentioned journals:


Antifungal and Antibacterial Activity of the Newly Synthesized 2-Xanthone Derivatives

A series of 2-substituted xanthone derivatives 8-20 containing selected allyl, cinnamyl, morpholine, and imidazole moieties were synthesized and tested for their antifungal and antibacterial in-vitro properties. Of the newly synthesized derivatives, ten revealed antifungal activity especially against Trichophyton mentagrophytes (the biggest inhibition zones ranged 35 mm for 11 and 13). 2-(3-(Allylamino)propoxy)-9H-xanthen-9-one hydrochloride 9 inhibited growth of all of the examined fungal species. Significant efficacy against evaluated yeasts and dermatophytes was also observed for 6-chloro-2-methyl-9H-xanthen-9-one derivatives 11-13 containing encyclic amine moieties. Additionally, compounds 9, 11, and 12 hindered development of bacteria species but in a lesser degree. They were efficacious against Staphylococcus aureus, Escherichia coli, and Enterococcus faecalis.

Source: Archiv der Pharmazie | 2 Dec 2008 | 5:24 am CET

Synthesis and Pharmacological Evaluation of N-(Dimethylamino)ethyl Derivatives of Benzo- and Pyridopyridazinones

New N-(dimethylamino)ethyl derivatives of phthalazinones and pyridopyridazinones 7, 9 were synthesized and assayed as potential analgesic agents in the hot-plate, tail-flick, and writhing tests. Pharmacological assay demonstrated that eight (in ten) of the newly synthesized compounds showed antinociceptive activity. Especially, 2-[2-(dimethylamino)ethyl]-4-phenyl-2H-phthalazin-1-one 7a showed remarkably higher antinociceptive activity in all tests. This is connected with influence on supraspinal, spinal, and peripheral structures. The decreased sensitivity to the pain stimulus in the hot-plate was higher than that of metamizole.

Source: Archiv der Pharmazie | 2 Dec 2008 | 5:24 am CET

Synthesis and Antimicrobial Activity of Some Novel 2-[4-(Substituted Piperazin-/Piperidin-1-ylcarbonyl)phenyl]-1H-benzimidazole Derivatives

In this study, we report the synthesis and antimicrobial evaluation of several new 4-(1H-benzimidazol-2-yl)benzamides (11-30) and 5-chloro-1-(p-fluorobenzyl)-2-{4-[(4-methylpiperazin-1-yl)carbonyl]phenyl}-1H-benzimidazole (33). Compound 20 exhibited the best antibacterial activity with MIC value of 6.25 [mu]g/mL against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA). Significant antifungal activities were obtained with the compounds 13, 14, 18, 19, and 33 with MIC values of 3.12 [mu]g/mL which are close to fluconazole.

Source: Archiv der Pharmazie | 2 Dec 2008 | 5:24 am CET

New 1H-Pyrazole-4-Carboxamides with Antiplatelet Activity

Nine title compounds were synthesized and investigated in the Born test for their antiplatelet activities against collagen, ADP, adrenaline, and platelet activating factor (PAF) as inducers of the aggregation. Using collagen three compounds with IC50 values below 100 [mu]M were found (3b, 3e, 3i). Activities in nanomolar concentrations were observed against ADP (3b, IC50 = 9.4 nM), adrenaline (3i, IC50 = 5.8 nM), and platelet activating factor (3e, IC50 = 0.45 nM).

Source: Archiv der Pharmazie | 2 Dec 2008 | 5:24 am CET

Determining Pyracetam in Parent Substance and Ready-to-Use Medicinal Forms by Differential Scanning Calorimetry

Analysis of pyracetam in available parent powders using differential scanning calorimetry (DSC) showed that there are at least two main polymorphic forms of pyracetam on the pharmaceutical market. One of these is converted into the other during heating and storage. Two polymorphic forms of pyracetam have been found in pyracetam capsules, in contrast to tablets where only one form is present. The results show that amorphization of crystalline active ingredient during heating of dosed forms including polyethyleneglycol or other carriers should be taken into account during analysis by means of DSC.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0143-5
  • Authors
    • A. V. Titova, Ministry of Public Health of the Russian Federation Institute for Drug Standardization, State Scientific Center for Drug Review and Control Moscow Russia
    • A. P. Arzamastsev, Sechenov Medical Academy Moscow Russia
    • D. Yu. Chashkin, Ministry of Public Health of the Russian Federation Institute for Drug Standardization, State Scientific Center for Drug Review and Control Moscow Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Synthesis and Antituberculosis Activity of 4-aminobenzenesulfamido-2-thiazole 8-benzodioxane Azomethines

The reactions of 4-(aminobenzenesulfonamide)-2-thiazole with the appropriate 8-benzodioxane aldehydes were used to synthesize a series of new azoethines. The proposed structures are confirmed by IR and NMR spectroscopy. It is shown that the obtained azomethines exhibit high (97–100%) activity against Mycobacterium tuberculosis H37Rv at a concentration of 0.2–1.5 mg-mL in vitro.

  • Content Type Journal Article
  • Category Search for New Drugs
  • DOI 10.1007/s11094-008-0135-5
  • Authors
    • R. T. Tlegenov, Berdakh Karakalpak State University Nukus Karakalpak Republic Uzbekistan

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Micro-Preparative Chromatographic Separation of Naproxen Enantiomers

Chromatographic micro-preparative separation of a racemic mixture of naproxen enantiomers using a chiral stationary phase of Chiralcel OJ-H has been studied. Optimum conditions for the separation have been found. It is shown that a special fraction collection scheme involving an intermediate region between the minimum between peaks and the maximum of the second peak should be used for the simultaneous recovery of both enantiomers. In this case, S-(0.12 mg) and R-naproxen (0.12 mg) with a purity of up to 99.4 and 94.5%, respectively, can be isolated in one run using a standard analytical column.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0145-3
  • Authors
    • L. D. Asnin, Russian Academy of Sciences Institute of Technical Chemistry, Ural Branch Perm Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Using Near-Infrared Spectrophotometry for the Identification of Pharmaceuticals and Drugs

The near infrared range (NIR) of the electromagnetic spectrum extends from 800 to 2500 nm, being confined between the middle IR and visible spectral regions. The method of NIR spectroscopy is based on a combination of spectrophotometry and statistical methods of multifactor analysis, which provides excellent possibilities for drug identification and quality control even without opening the package. We have studied a series of drugs including cefazolin sodium and generic drugs based on enalapril maleate. True and falsified variants of a given drug X were classified into groups according to “drug name,” “drug manufacturer,” and “falsified product” by means of NIR spectroscopic analyses performed using the NIR Fourier-transform instruments Multi Purpose Analyzer (Bruker, Germany) and Antaris (Thermo Electron Corporation, USA). The potential of this method for the identification of drugs without violation of their packing shows good prospects for introducing it into the drug quality control system. This method should be recommended for introduction into the future Russian State Pharmacopoeia as a general method of drug analysis.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0146-2
  • Authors
    • T. E. Elizarova, FARMANALIZ Analytical Control Laboratory Moscow Russia
    • S. V. Shtyleva, FARMANALIZ Analytical Control Laboratory Moscow Russia
    • T. V. Pleteneva, Peoples Friendship University Medical Faculty Moscow Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Imidazole Derivatives. XXX. Synthesis and Antitumor Activity of 4-amyloxy-3-nitroacetophenone 2-imidazolinyl-2-hydrazone and Related Compounds

The antitumor properties of 2-imidazolinyl-2-hydrazones of acetophenones with various substituents in the benzene ring have been studied. High activity is found for 4-amyloxy-3-nitroacetophenone 2-imidazolinyl-2-hydrazone, which points to the expediency of its further investigation.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0133-7
  • Authors
    • M. A. Iradyan, National Academy of Sciences of Armenia Mndzhoyan Institute of Fine Organic Chemistry Yerevan Armenia
    • R. A. Aroyan, National Academy of Sciences of Armenia Mndzhoyan Institute of Fine Organic Chemistry Yerevan Armenia
    • G. M. Stepanyan, National Academy of Sciences of Armenia Mndzhoyan Institute of Fine Organic Chemistry Yerevan Armenia
    • F. G. Arsenyan, National Academy of Sciences of Armenia Mndzhoyan Institute of Fine Organic Chemistry Yerevan Armenia
    • B. T. Garibdzhanyan, National Academy of Sciences of Armenia Mndzhoyan Institute of Fine Organic Chemistry Yerevan Armenia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Swelling, Erosion, and Release Behavior of PEO/Primaquine Matrix Tablets

Extended-release primaquine tablets were developed using polyethylene oxide (PEO) as a hydrophilic swellable polymer with different amounts and molecular weights (4 × 106 and 8 × 106). Investigations were carried out in order to verify the matrix performance. The evaluated parameters were weight, hardness, thickness, friability, and drug content. The swelling and erosion matrices as well as drug release profile were analyzed under dissolution conditions. The statistical model ANOVA and Tukey-Kramer HSD were considered. The results showed that all formulations provided adequate physical characteristics and a time release about eight hours following a non-Fickian diffusion model. The kinetics of drug delivery was directly related to the synchronization of swelling and erosion matrices. The formulations prepared with high PEO concentrations showed a lower rate of erosion, a slower drug release, and faster rate of swelling, as compared with matrices containing lower PEO concentration.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0137-3
  • Authors
    • A. P. Cruz, Universidade Federal de Santa Catarina Departament of Pharmaceutical Sciencs Florianópolis SC Brazil
    • C. D. Bertol, Universidade Federal de Santa Catarina Departament of Pharmaceutical Sciencs Florianópolis SC Brazil
    • H. K. Stulzer, Universidade Federal de Santa Catarina Departament of Pharmaceutical Sciencs Florianópolis SC Brazil
    • F. S. Murakami, Universidade Federal de Santa Catarina Departament of Pharmaceutical Sciencs Florianópolis SC Brazil
    • F. T. Costella, Universidade Federal de Santa Catarina Departament of Pharmaceutical Sciencs Florianópolis SC Brazil
    • H. V. A. Rocha, Fundação Oswaldo Cruz, Fiocruz Departament of Pharmaceutical Technology Rio de Janeiro RJ Brazil
    • M. A. S. Silva, Universidade Federal de Santa Catarina Departament of Pharmaceutical Sciencs Florianópolis SC Brazil

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Adsorptive Stripping Voltammetric Determination of Irbesartan in Bulk and Pharmaceutical Products

Adsorptive stripping Voltammetric determination of irbesartan using a hanging mercury drop electrode (HMDE) is described. The method is based on adsorptive accumulation of the species at the HMDE, followed by a first-harmonic alternating current (AC) stripping sweep at pH 6. The behavior of the adsorptive stripping response was studied under various experimental conditions, e.g., type of supporting electrolyte, pH, accumulation time, scan rate, and mode of sweep. In Britton-Robinson buffer solution, a quasi-reversible reduction process involving transfer of two electrons and two protons takes place. The response was linear over the concentration range of 0.16–1.60 µg/ml with regression coefficient 0.997 and detection limit 0.11 µg/ml. The average of determinations of the cited compound in oral dosages with its standard deviation was 99.39 ± 4.33 %.The result obtained by the proposed method was compared with that obtained by the uv-spectrophotometric technique. Furthermore, the proposed method was also successfully applied as a stability-indicating method.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0144-4
  • Authors
    • I. H. I. Habib, National Research Centre, Dokki Applied Organic Chem. Dept. Cairo Egypt
    • S. A. Weshahy, Cairo University Anal. Chem. Dept., Faculty of Pharmacy Cairo Egypt
    • S. Toubar
    • M. M. A. El-Alamin, Helwan University Anal. Chem. Dept., Faculty of Pharmacy Cairo Egypt

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Comparison of Acid-Neutralizing Properties of Anti-Acid Preparations of Various Compositions

The acid-neutralizing properties of widely used antacid preparations and the new experimental tablets Antacid-1 and Antacid-2 containing activated charcoal were compared in vitro. It is established that the new medicinal antacids differ from the well-known analogs by a greater acid-neutralizing capacity and a higher rate of hydrochloric acid neutralization.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0139-1
  • Authors
    • D. D. Grinshpan, Belarus State University Research Institute for Physico-Chemical Problems Minsk Belarus
    • T. N. Nevar, Belarus State University Research Institute for Physico-Chemical Problems Minsk Belarus
    • T. A. Savitskaya, Belarus State University Minsk Belarus
    • A. V. Boiko, Belarus State University Minsk Belarus
    • N. V. Kapralov, Belarus State Medical University Minsk Belarus
    • I. A. Sholomitskaya, Belarus State Medical University Minsk Belarus

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Quality Control Methods for Group D Vitamins

Determination of the content of vitamin D is a rather difficult problem. In the present study, we have compared methods that are most widely used for determining group D vitains. In recent years, physical and chemical methods of analysis have found increasing use due to their simplicity, sensitivity, and information value. Various methods of quality control are currently used but the future in the analysis of calciferols undoubtedly belongs to HPLC. This method is capable of simultaneously solving all problems encountered in the analysis of group D vitamins.

  • Content Type Journal Article
  • Category Structure of Chemical Compounds, Methods of Analysis and Process Control
  • DOI 10.1007/s11094-008-0140-8
  • Authors
    • O. V. Rybakova, Voronezh State University Novonezh Russia
    • E. F. Safonova, Voronezh State University Novonezh Russia
    • A. I. Slivkin, Voronezh State University Novonezh Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Synthesis and Antimicrobial Activity of Complexes Based on 4-aryl-2-hydroxy-4-oxo-2-butenoic Acid N -heterylamides

Reaction of 4-aryl-2-hydroxy-4-oxo-2-butenoic acid N-hetarylamides with copper, zinc, and cadmium dichlorides led to the formation of bis[3-aryl-1-(N-hetaryl)carboxamido-1,3-propanedionato]copper,-zinc, and-cadmium, respectively. Compounds with high antimicrobial activity were found among these products.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0147-1
  • Authors
    • N. A. Pulina, Perm State Pharmaceutical Academy Perm Russia
    • P. A. Mokin, Perm State Pharmaceutical Academy Perm Russia
    • V. V. Yushkov, Perm State Pharmaceutical Academy Perm Russia
    • V. V. Zalesov, Perm State University Perm Russia
    • T. F. Odegova, Perm State Pharmaceutical Academy Perm Russia
    • M. V. Tomilov, Perm State Pharmaceutical Academy Perm Russia
    • K. V. Yatsenko, Perm State Pharmaceutical Academy Perm Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Mucoadhesive Drug Delivery Systems: Quantitative Assessment of Interaction Between Synthetic and Natural Polymer Films and Mucosa

A method for evaluating mucoadhesive properties of polymer films that employs a model mucosa and wetting of tissues imitating physiological conditions is proposed. The results show evidence for good mucoadhesive properties of natural biocompatible polymers such as alginate and chitosan. The proposed method can be used to compare the mucoadhesive strength of various polymers widely used in pharmaceutical technology.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0132-8
  • Authors
    • E. A. Kharenko, Sechenov Moscow Medical Academy Department of Pharmacy 119881 Moscow Russia
    • N. I. Larionova, Moscow State University Department of Chemistry 119992 Moscow Russia
    • N. B. Demina, Sechenov Moscow Medical Academy Department of Pharmacy 119881 Moscow Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Experimental Adaptation of Staphylococcus Aureus to Sulfuryl Derivatives of Benzazolides

A state of pre-adaptation to highly toxic doses of sulfuryl derivatives of benzimidazole and benzotriazole was developed in Staphylococcus aureus species by treating them with non-toxic doses of these compounds. Pre-treatment of S. aureus with the starting benzazolides (benzimidazole and benzotriazole) also created the pre-adaptation to their sulfuryl derivatives. Experiments on cross-pre-adaptation where the pre-adaptation to sulfuryl derivatives of benzazolides was created by the action of non-toxic doses of benzotriazole and vice versa showed that the planar structures of the double ring of benzazolide plays a key role in activation of the repair systems of S. aureus. Mathematical analysis revealed a high nonlinear correlation between the ability of a compound to create the state of pre-adaptation in S. aureus culture on one hand and the physical and chemical properties such as the lipophilicity, molecular weight and volume, and hydration energy on the other.

  • Content Type Journal Article
  • Category Molecular-Biological Problems of Drug Design and Mechanism of Drug Action
  • DOI 10.1007/s11094-008-0136-4
  • Authors
    • E. S. Selezneva, Samara State University Samara Russia
    • E. I. Ten’gaev, Samara State University Samara Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Synthesis, Influence on Blood Coagulation and Antimicrobial Activity of 2-arylaminocinchoninic Acid Pyridinioacetylhydrazide Chlorides

Chlorides of 2-arylaminocinchoninic acid pyridinioacetylhydrazides were synthesized via interaction of the chloroacetylhydrazides of these acids with pyridine and its derivatives. These compounds showed antimicrobial activity and influenced blood coagulation.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0134-6
  • Authors
    • M. E. Kon’shin, Perm State Pharmaceutical Academy Perm Russia
    • B. Ya. Syropyatov, Perm State Pharmaceutical Academy Perm Russia
    • A. L. Efremov, Perm State Pharmaceutical Academy Perm Russia
    • T. F. Odegova, Perm State Pharmaceutical Academy Perm Russia
    • M. M. Vakhrin, Perm State Pharmaceutical Academy Perm Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Experimental Evaluation of the Chemotherapeutic Efficacy and Toxicity of a New Medicinal Form of Dioxidine: Lidoxycol Ointment

The antibacterial activity in vitro and in vivo and the toxicity of Lidoxycol ointment, which is a new medicinal form of dioxidine, have been studied in comparison to the properties of Dioxycol ointment. The results showed that Lidoxycol is identical to Dioxycol with respect to the spectrum of antimicrobial action, chemotherapeutic efficiency, and tolerance.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0141-7
  • Authors
    • T. V. Pushkina, All-Russia Research Institute of Pharmaceutical Chemistry Center for Drug Chemistry Moscow Russia
    • L. Yu. Krylova, All-Russia Research Institute of Pharmaceutical Chemistry Center for Drug Chemistry Moscow Russia
    • S. A. Sharova, All-Russia Research Institute of Pharmaceutical Chemistry Center for Drug Chemistry Moscow Russia
    • L. A. Chicherina, All-Russia Research Institute of Pharmaceutical Chemistry Center for Drug Chemistry Moscow Russia
    • O. S. Kuzina, All-Russia Research Institute of Pharmaceutical Chemistry Center for Drug Chemistry Moscow Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Method for Identification of the New X-Ray Contrast Agent Yttrium Orthotantalate

Conditions have been chosen for the decomposition of yttrium orthotantalate and the subsequent determination of yttrium and tantalum in this compound, which is used as an x-ray contrast agent. Methods are developed for the identification of yttrium and tantalum using complexation reactions. These methods have proven to be specific and can be recommended for the identification of yttrium and tantalum in the new preparation of yttrium orthotantalate 3% suspension for use in x-ray fluorography. Infrared spectroscopy can be used to confirm the identity of yttrium orthotantalate in the studied pharmacological agent.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0142-6
  • Authors
    • E. A. Mamashina, State Scientific Center for Drug Review and Control Institute for Drug Standardization Moscow Russia
    • T. N. Bokovikova, State Scientific Center for Drug Review and Control Institute for Drug Standardization Moscow Russia
    • E. P. Gernikova, State Scientific Center for Drug Review and Control Institute for Drug Standardization Moscow Russia

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Comparative Study of the Adsorption Activity of Medicinal Sorbents

A comparative study of the adsorption activity of some medical sorbents with respect to physiologically active substances with different molecular weights has been carrried out. It is shown that Siliks (Polysorb MP) exhibits greater ability to adsorb proteins in comparison to other sorbents. In contrast, the carbon-based sorbents do not absorb proteins but have a high affinity for low-and medium-molecular-weight substances. The adsorption activity of Smecta in acid media is close to that of carbons. Due to similar chemical properties, the Siliks and Enterosgel preparations demonstrate analogous adsorption characteristics.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0138-2
  • Authors
    • D. A. Markelov, A. A. Bogomolets National Medical University Kiev Ukraine
    • O. V. Nitsak, A. A. Bogomolets National Medical University Kiev Ukraine
    • I. I. Gerashchenko, National Academy of Sciences of Ukraine Institute of Surface Chemistry Kiev Ukraine

Source: Pharmaceutical Chemistry Journal | 26 Nov 2008 | 9:09 pm CET

Synthesis, Antiplatelet and Vasorelaxing Activities of Xanthone Derivatives

A series of [omega]-aminoalkoxylxanthones was synthesized and tested in vitro for their ability to inhibit platelet aggregation and cause vasorelaxing action. Compounds 4, 5, 12, 17, and 18 showed significant antiplatelet effects on thrombin-, arachidonic acid (AA)-, collagen-, and platelet activating factor (PAF)-induced washed rabbit platelet aggregation and exhibited inhibition of primary and secondary aggregation induced by adenosine-5'-diphosphate (ADP) in human platelet-rich-plasma (PRP). Compounds 4, 17, and 18 revealed vasorelaxing activities in rat thoracic aorta. We concluded that these compounds may be developed as new antithrombotic agents.

Source: Archiv der Pharmazie | 26 Nov 2008 | 3:08 am CET

Synthesis and Anticonvulsant Activity of New N-(Alkyl/Sub-stituted aryl)-N[prime]-[4-(5-cyclohexylamino)-1,3,4-thiadiazole-2-yl)phenyl]thioureas

A series of novel thiourea derivatives carrying the 5-cylohexylamino-1,3,4-thiadiazole moiety was synthesized and their anticonvulsant activity was evaluated. Structures of the synthesized compounds have been confirmed by IR, 1H-NMR, and elemental analysis. All of the compounds were administered at a dose of 50 mg/kg. Some of the active compounds have different effects in pentylenetetrazole (PTZ) and maximal electroshock (MES) tests, indicating the therapeutical potential in petit mal seizures, but not in grand mal seizures. Compounds 10, 11, 13, and 14 carrying 2-methylphenyl, 4-chlorophenyl, allyl, and 4-methylphenyl on the thiourea pharmacophore, increased the survival rate in the PTZ model. The ED50 values of the active compounds 10, 11, 13, and 14 were found 68.42, 43.75, 18.75 and 25 mg/kg, respectively.

Source: Archiv der Pharmazie | 26 Nov 2008 | 3:08 am CET

Synthesis and biological evaluation of substituted thiophenyl derivatives of indane-1,3-dione

Abstract  Indane-1,3-dione (1) synthesized by condensation of diethyl phthalate and ethyl acetate in the presence of sodium ethoxide gave the sodium salt of the ester derivative, which on neutralization in the presence of sulfuric acid afford 1. Various thiols were converted to disulfide (3) which on treatment with 1 gave 2-substituted thiophenyl derivatives (4a–g) of 1. The synthesized compounds were characterized on the basis of IR and 1H NMR. The synthesized compounds (4a–g) were investigated for their anticoagulant, analgesic, anti-inflammatory, antifungal, antibacterial, and anticancer activities. Some of the synthesized compounds have shown moderate activities.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0120-z
  • Authors
    • D. Giles, K. M. College of Pharmacy Madurai India
    • M. S. Prakash, K. M. College of Pharmacy Madurai India
    • K. V. Ramseshu, K. M. College of Pharmacy Madurai India

Source: Pharmaceutical Chemistry Journal | 13 Nov 2008 | 5:06 pm CET

Antianemic activity of polymetallocomplexes of pectin polysaccharides with Fe2+, Co2+, and Cu2+ with different ratios of d metals

Abstract  The antianemic activity of water-soluble polymetallocomplexes of pectin polysaccharides containing d metal ions — Fe2+, Co2+, and Cu2+ — at different ratios was studied in laboratory rats. The results showed that complexes had marked stimulatory effects on hematopoietic processes, with increases in hemoglobin concentrations and erythrocyte counts, along with intensification of the recovery of hematological parameters after anemia induced by hemorrhage. The highest level of activity on hematological measures was obtained with the polymetallocomplex containing Fe2+, Co2+, and Cu2+ ions at a ratio close to 1:1:1.

  • Content Type Journal Article
  • Category The Search for New Therapeutic Substances
  • DOI 10.1007/s11094-008-0130-x
  • Authors
    • A. B. Vyshtakalyuk, A. E. Arbuzov Institute of Organic and Physical Chemistry Kazan Russia
    • A. N. Karaseva, A. E. Arbuzov Institute of Organic and Physical Chemistry Kazan Russia
    • V. V. Karlin, A. E. Arbuzov Institute of Organic and Physical Chemistry Kazan Russia
    • S. T. Minzanova, A. E. Arbuzov Institute of Organic and Physical Chemistry Kazan Russia
    • V. F. Mironov, A. E. Arbuzov Institute of Organic and Physical Chemistry Kazan Russia
    • A. I. Konovalov, A. E. Arbuzov Institute of Organic and Physical Chemistry Kazan Russia

Source: Pharmaceutical Chemistry Journal | 13 Nov 2008 | 5:06 pm CET

Synthesis and antimicrobial activity of sulfanilamide-containing copper (II) naphthalidenethiosemicarbazidates

Abstract  Aseries of copper (II) streptocide-, sulfacyl-, norsulfazole-, ethazole-, and sulfadimezine-containing naphthalidenethiosemicarbazidates and napthalidene-4-phenylthiosemicarbazidates with high levels of antimicrobial activity were synthesized. Elemental analysis, magnetochemical, IR spectroscopic, and thermogravimetric data were used to confirm the compositions and structures of the resulting complexes. The effects of the nature of the central atom and the influences of the sulfanilamide and phenyl radicals in the azomethine thiosemicarbazone fragment on the antimicrobial activity of the compounds against 10 strains of Gram positive and Gram negative microorganisms were studied. The most active of the compounds synthesized were the copper norsulfazole-, ethazole-, and sulfadimezine-containing naphthalidenethiosemicarbazidates.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0118-6
  • Authors
    • A. P. Gulya, Moldova State University Kishinev Moldova
    • V. I. Prisakar, N. Testemitsan State University of Medicine and Pharmacy Kishinev Moldova
    • V. I. Tsapkov, Moldova State University Kishinev Moldova
    • S. A. Buracheva, N. Testemitsan State University of Medicine and Pharmacy Kishinev Moldova
    • S. N. Spynu, Moldova State University Kishinev Moldova
    • N. P. Bezhenar, Moldova State University Kishinev Moldova

Source: Pharmaceutical Chemistry Journal | 13 Nov 2008 | 5:06 pm CET

Antibacterial, antifungal, antiherbicidal, and antifungicidal activity of 4,6-dimethoxyhomophthalic acid and related compounds

Abstract  4,6-Dimethoxyhomophthalic acid (5) has been synthesized efficiently in four steps from 3,5-dimethoxycinnamic acid (1) and characterized and screened for their in vitro antibacterial activity against four Gram negative (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhii, and Shigella flexneri) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains, and for in vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glaberata. The compounds were screened for their in vitro antiherbicidal and antifungicidal activities.

  • Content Type Journal Article
  • DOI 10.1007/s11094-008-0121-y
  • Authors
    • Ghulam Qadeer, Quaid-I-Azam University Department of Chemistry Islamabad 45320 Pakistan
    • Nasim Hasan Rama, Quaid-I-Azam University Department of Chemistry Islamabad 45320 Pakistan
    • Muhammad Zareef, Quaid-I-Azam University Department of Chemistry Islamabad 45320 Pakistan
    • Najim A. Al-Masoudi, Universität Konstanz Formerly Fachbereich Chemie Postfach 5560, M-655 D-78457 Konstanz Germany

Source: Pharmaceutical Chemistry Journal | 13 Nov 2008 | 5:06 pm CET




 


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Internetchemie ? 2007 - 2008 A. J.