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Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
Medicinal Chemistry Research | Year: 2013

In an attempt to find new agents to fight against microbial infections, a series of coumarin-based 1,3,4-oxadiazol-2ylthio-N-phenyl/benzothiazolyl acetamides was synthesized starting from coumarin-3-carboxylic acid ethyl ester obtained through Knoevenagel and Pinner reaction. In vitro antimicrobial activity against several bacteria (S. aureus, B. cereus, E. coli, P. aeruginosa, K. pneumoniae, S. typhi, P. vulgaris, S. flexneri), fungi (A. niger, A. fumigatus, A. clavatus, C. albicans) and antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain was assessed. This study shows to what extent the presence of various electron withdrawing/donating substituents on the phenyl or benzothiazole ring affects the activity profiles of the newer molecules. The relationship between activity profiles (MICs, 3.12-25 μg/mL) and the lipophilic character (LogP) of the prepared products is also discussed and the MIC values of the active conjugates seem to correlate to some extent with the lipophilicity profiles. Two (5e and 6c) of the final analogues displayed promising antimycobacterial activity at 12.5 μg/mL of MIC, half fold potent to the standard drug pyrazinamide (6.25 μg/mL). Compounds were characterized by IR, 1H NMR, 13C NMR spectroscopy and elemental analysis. © 2012 Springer Science+Business Media, LLC. Source


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Patel P.K.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
European Journal of Medicinal Chemistry | Year: 2012

To affiliate multiple bioactivities in a compact heteronuclei, two series of benzimidazole based 1,3,4-oxadiazoles were synthesized and assessed in vitro for their efficacy as antimicrobial agents against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneri), four fungi (Aspergillus niger, Aspergillus fumigatus, Aspergillus clavatus, Candida albicans) and Mycobacterium tuberculosis H37Rv and best results were observed amongst the N-benzothiazolyl aetamide series. The lipophilicity (LogP) influence on the biological profile (MICs) of the prepared products was also discussed. Upon biological screening, it was observed that the majority of the compounds were found to possess a significant broad spectrum antimicrobial (3.12-25 μg/mL of MIC) and antitubercular (6.25-25 μg/mL of MIC) potential. The structural assignments of the new products were done on the basis of IR, 1H NMR, 13C NMR spectroscopy and elemental analysis. © 2012 Elsevier Masson SAS. All rights reserved. Source


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Pannecouque C.,Rega Institute for Medical Research | And 2 more authors.
Future Medicinal Chemistry | Year: 2012

Background: The acquirement of resistance by microorganisms to the antimicrobial arsenal is a threat to public health. A recent WHO report estimated that 1.3 million HIV-negative people and 0.38 million HIV-positive people died from TB in 2009. Various forms of cancer account for a high percentage of deaths in both women (breast cancer) and men (prostate cancer). Results & discussion: In vitro activity assessment of newly constructed s-triazines against a panel of microorganisms including bacteria, fungi and Mycobacteria demonstrated that the compounds are of immense attraction for impending drug discovery. They were further examined for in vitro activity against breast cancer and prostate cancer cell lines, as well as HIV-1 (III B) and HIV-2 (ROD) viral strains. Proposed structural confirmation studies by IR, H NMR, 13C NMR, 19F NMR spectroscopy and elemental analysis were in accordance. Conclusion: Activity profiles of the products may contribute considerably to future drug-discovery studies. © 2012 Future Science Ltd. Source


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
Journal of Fluorine Chemistry | Year: 2011

A series of 2-[4-cyano-(3-trifluoromethyl)phenyl amino)]-4-(4-quinoline/ coumarin-4-yloxy)-6-(fluoropiperazinyl)-s-triazines has been synthesized by a simple and efficient synthetic protocol. The antimicrobial activity of the compounds was studied against several bacteria (Staphylococcus aureus MTCC 96, Bacillus cereus MTCC 619, Escherichia coli MTCC 739, Pseudomonas aeruginosa MTCC 741, Klebsiella pneumoniae MTCC 109, Salmonella typhi MTCC 733, Proteus vulgaris MTCC 1771, Shigella flexneria MTCC 1457) and fungi (Aspergillus niger MTCC 282, Aspergillus fumigatus MTCC 343, Aspergillus clavatus MTCC 1323, Candida albicans MTCC 183) using paper disc diffusion technique and agar streak dilution method. Newly synthesized compounds were also tested for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using BACTEC MGIT and Lowenstein-Jensen MIC method. © 2011 Elsevier B.V. Source


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
European Journal of Medicinal Chemistry | Year: 2011

A series of novel s-triazine analogs were synthesized and characterized by IR, 1H NMR, 13C NMR, 19F NMR spectroscopy and elemental analysis. Preliminary screening of target compounds against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneria), four fungi (Aspergillus niger, Aspergillus fumigatus, Aspergillus clavatus, Candida albicans) and Mycobacterium tuberculosis H37Rv indicated that 5d, 5h, 5n, 5p, 5q, 5r, 5s, 5t and 5u were the most active compounds among twenty one studied. Thus, they were further subjected to in vitro biological evaluation against human prostate cancer cell line (DU-145) and the results indicate that two compounds 5n and 5s were markedly active. © 2011 Elsevier Masson SAS. All rights reserved. Source

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