Synthesis of some Novel N-Aryl-1,4-Dihydropyridines Derivatives and Their Biological Evaluation as Potential Antimycobaceterial Agents

Authors(1) :-Amish P. Khamar

Tuberculosis, due to its unyielding nature, is now a chief civic health threat. The associated renaissance of TB with the MDR or XDR-TB and HIV/AIDS epidemic has exposed the infirmities of the current drug armatorium. Recent studies showed that 1,4-dihydropyridine-3,5-dicarbamoyl derivatives with lipophilic groups have significant antitubercular activity. We have synthesized new N-aryl-1,4-dihydropyridines bearing carbethoxy and acetyl group at C-3 and C-5 of the DHP ring. In addition, 1H-pyrazole ring is substitutes at C-4 position. The in vitro antitubercular activity of compounds against Mycobacterium tuberculosis H37Rv was evaluated. The lowest minimum inhibitory concentration value, 0.02 g/mL, was found for diethyl 1-(2-chlorophenyl)-1,4-dihydro-2,6-dimethyl-4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine-3,5-dicarboxylate 4e making it more potent than first line antitubercular drug isoniazid. In addition, this compound exhibited relatively low cytotoxicity.

Authors and Affiliations

Amish P. Khamar
Arts, Science & R. A. Patel Commerce College, Bhadran, Gujarat, India

1, 4-Dihydropyridines, Antitubercular Activity, Antimycobacterial Activity, Mycobacterium Tuberculosis.

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Publication Details

Published in : Volume 1_ | Issue 1 | 2014
Date of Publication : 2014-12-30
License:  This work is licensed under a Creative Commons Attribution 4.0 International License.
Page(s) : 174-182
Manuscript Number : IJSRSET184102
Publisher : Technoscience Academy

Print ISSN : 2395-1990, Online ISSN : 2394-4099

Cite This Article :

Amish P. Khamar, " Synthesis of some Novel N-Aryl-1,4-Dihydropyridines Derivatives and Their Biological Evaluation as Potential Antimycobaceterial Agents, International Journal of Scientific Research in Science, Engineering and Technology(IJSRSET), Print ISSN : 2395-1990, Online ISSN : 2394-4099, Volume 1_, Issue 1, pp.174-182, -2014.
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