We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Synthesis and Biological Evaluation of Some Novel 1,4-Dihydropyridines as Potential AntiTubercular Agents.
- Authors
Trivedi, Amit; Dodiya, Dipti; Dholariya, Bipin; Kataria, Vipul; Bhuva, Vimal; Shah, Viresh
- Abstract
Recent studies showed that 1,4-dihydropyridine-3,5-dicarbamoyl derivatives with lipophilic groups have significant antitubercular activity. In this study, we have synthesized new derivatives of 1,4-dihydropyridines bearing carbmethoxy and carbethoxy group at C-3 and C-5 of the 1,4-dihydropyridine ring. In addition, 1 H-pyrazole ring is substituted at C-4 position. These analogues were synthesized by multi-component Hantzsch reaction. The in vitro antitubercular activity of compounds against Mycobacterium tuberculosis H37Rv was evaluated. The lowest minimum inhibitory concentration value, 0.02 μg/mL and SI > 500, was found for dimethyl 1,4-dihydro-4-(3-(4-nitrophenyl)-1-phenyl-1 H-pyrazol-4-yl)-2,6-dimethylpyridine-3,5-dicarboxylate 3f, diethyl 1,4-dihydro-4-(3-(4-fluorophenyl)-1-phenyl-1 H-pyrazol-4-yl)-2,6-dimethylpyridine-3,5-dicarbo-xylate 4c and diethyl 1,4-dihydro-4-(3-(4-bromophenyl)-1-phenyl-1 H-pyrazol-4-yl)-2,6-dimethyl pyridine-3,5-dicarboxylate 4e, making them more potent than first-line antitubercular drug isoniazid. In addition, these compounds exhibited relatively low cytotoxicity.
- Subjects
PROTEIN synthesis; DIHYDROPYRIDINE; ANTITUBERCULAR agents; DRUG lipophilicity; MYCOBACTERIUM tuberculosis; ISONIAZID; CELL-mediated cytotoxicity
- Publication
Chemical Biology & Drug Design, 2011, Vol 78, Issue 5, p881
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/j.1747-0285.2011.01233.x