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Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research | Haswani N.G.,Rc Patel Institute Of Pharmaceutical Education And Research
Journal of Saudi Chemical Society

In an attempt to find a new class of antimicrobial agents, a series of thienopyrimidin-4(3H)-thiones 4(H1-H36) were synthesized and evaluated for in vitro antifungal activity against Candida albicans (NCIM 3471), Aspergillus niger (NCIM 545), and Penicillium chrysogenum (NCIM 709). The title compounds were synthesized by thionation of thienopyrimidin-4(3H)-ones 3(H1-H36) using Lawesson's reagent. All the compounds were characterized using elemental analytical (C, H, and N) and spectral (FT-IR, 1H NMR, 13C NMR and MS) data. Among the tested compounds, 5-(4-chlorophenyl)-2-(pyridin-3-yl)thieno[2,3-d]pyrimidine-4(3H)-thione 4(H11), 2-sulfanyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-4(3H)-thione 4(H18), and 2-(butylsulfanyl)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-4(3H)-thione 4(H32) were identified as potentially excellent antifungal agents. They exhibited potent antifungal activity against C. albicans (MIC; 4 μg/mL), A. niger (MIC; 2 μg/mL), and P. chrysogenum (MIC; 2 μg/mL) comparable with that of ketoconazole. The binding mode of compounds by SP docking studies shows that it fits well into the active site cavity of DHFR. Lipinski's rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use thereby indicating their potential as drug-like molecules. © 2014. Source

Patil P.O.,Rc Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research
Arabian Journal of Chemistry

The present review highlights the synthetic methods of monoamine oxidase inhibitors (MAO) belonging to a group of nitrogen heterocycles such as pyrazoline, indole, xanthine, oxadiazole, benzimidazole, pyrrole, quinoxaline, thiazole and other related compounds (1990-2012). Moreover, it emphasizes salient findings related to chemical structures and the bioactivities of these heterocycles as MAO inhibitors. The aim of this review is to find out different methods for the synthesis of nitrogen containing heterocycles and their bioactivity related aspects as MAO inhibitors. © 2013. Source

Firake S.D.,Rc Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research
Current Enzyme Inhibition

Benzenesulfonamide is versatile motif employed for the discovery in the field of medicinal and pharmaceutical chemistry. Over the years of active research, sulfonamide has evolved as important privileged pharmacophore in medicinal chemistry, encompassing a diverse range of biological activities including antiviral, carbonic anhydrase inhibitors, diuretic, and a protease inhibitor, hypoglycemic, anticancer and anti-inflammatory. On the other hand, owing to the fast development of new drugs possessing sulfonamide pharmacophore many research reports generated in a short span of time. Thus, there is a need to couple the most recent data with the prior data to comprehend the present status of benzenesulfonamide as anti-inflammatory agent. The present review highlights the molecular modeling and synthetic methods of benzenesulfonamide scaffold bearing various heterocyclic or carbocyclic rings such as thiazole, triazole, imidazole, isoxazoline, pyridine, pyranone, pyridazone, pyrimidine, pyran, indole, benzothiazole, benzotriazole, benzimidazole and benzopyran as central ring scaffold. In addition to this, the manuscript will be a guideline to medicinal chemists for rationally designing a novel benzenesulfonamide bearing compounds as COX-2 inhibitors. © 2015 Bentham Science Publishers. Source

Redasani V.K.,Rc Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research
Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry

The present work is an agreement with simple and efficient method of improving the therapeutic efficacy of ibuprofen by masking its acidic moiety. It aims to reduce gastrointestinal side effects by controlling the rate, duration and site of release. This is achieved by synthesis and evaluation of polymeric prodrug of ibuprofen with natural polymer sodium alginate. The synthesis was supported by N-protected serine as spacer due to chemical incompatibility of drug and polymer. Synthesized prodrug was characterized for confirmation of said structures. The in-vitro dissolution profile of ibuprofen-alginate prodrug showed that the release of the drug is significantly higher in case of pH 7.2 buffer as compared to ibuprofen, which might be due to ester group adjacent to drug get hydrolyzed. The hydrolysis was found to be with faster rate in alkaline media than that of in acidic media. © 2015 Bentham Science Publishers. Source

Zawar L.R.,H R Patel Institute Of Pharmaceutical Education And Research | Bhandari G.S.,R C Patel Institute Of Pharmacy | Bari S.B.,Hr Patel Institute Of Pharmaceutical Education And Research
Research Journal of Pharmaceutical, Biological and Chemical Sciences

The monolithic matrix type transdermal films of Lovastatin (LS) were prepared by film casting technique on mercury substrate. Nine formulations were developed using Eudragit RL 100 (ERL) with Eudragit RS 100 (ERS) in ratio of 4:1 with oleic acid (OA) and menthol (MN) as penetration enhancers, alone or combination and were coded as G1, G2 G3, G4, G5, G6, G7, G8 and G9. All the formulations carried 10% w/w of Lovastatin and 30% w/w of Dibutyl Phthalate (DBP) in Chloroform as solvent system. The films were evaluated for physicochemical and in vitro diffusion studies using Keshary-Chien diffusion cell. All the films were found to be suitable for formulating in terms of physicochemical characteristics. The corresponding values for cumulative drug permeation for said formulation were 284.55 (G1), 283.88 (G2), 290.85 (G3), 297.12 (G4), 311.89 (G5), 353.95 (G6), 443.60 (G7), 312.98 (G8) and 356.68 (G9) mcg/cm 2. On the basis of in vitro permeation studies formulation G7 was having maximum rate of permeation and it was selected as optimized formulation. The correlation coefficient obtained from Higuchi plot was found to be in the range of 0.95 to 0.99 indicating that diffusion mechanism of drug release. Drug-excipient interaction studies were carried out using TLC and FTIR technique; films indicated no chemical interaction between drug and excipients. Primary skin irritation study shows the films are non irritant. Source

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