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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, 1H-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 H(37) Rv 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-1H-pyrazol-4-yl)-2,6-dimethylpyridine-3,5-dicarboxylate 3f, diethyl 1,4-dihydro-4-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)-2,6-dimethylpyridine-3,5-dicarboxylate 4c and diethyl 1,4-dihydro-4-(3-(4-bromophenyl)-1-phenyl-1H-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.

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N-Aryldihydropyrimidines (IV), bearing an acetyl or a carbethoxy group at the 3-and 5-position of the dihydropyridine ring and a pyrazole ring at position 4, are synthesized to overcome the resistant isolates. Comparison of the in vitro antitubercular activities of the preliminarily screened compounds indicates that (IVg) is more potent than the first line antitubercular drug isoniazid. Compound (IVg) shows relatively low cytotoxicity. -(TRIVEDI*, A. R.; DODIYA, D. K.; DHOLARIYA, B. H.; KATARIA, V. B.; BHUVA, V. R.; SHAH, V. H.; Bioorg. Med. Chem. Lett. 21 (2011) 18, 5181-5183, http://dx.