Antituberculosis: synthesis and antimycobacterial activity of novel benzimidazole derivatives.

ABSTRACT: A total of seven novel benzimidazoles were synthesized by a 4-step reaction starting from 4-fluoro-3-nitrobenzoic acid under relatively mild reaction conditions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H??Rv (MTB-H??Rv) and INH-resistant M. tuberculosis (INHR-MTB) strains using agar dilution method. Three of them displayed good activity with MIC of less than 0.2??M. Compound ethyl 1-(2-(4-(4-(ethoxycarbonyl)-2-aminophenyl)piperazin-1-yl)ethyl)-2-(4-(5-(4-fluorophenyl)pyridin-3-ylphenyl-1H-benzo[d]imidazole-5-carboxylate (5 g) was found to be the most active with MIC of 0.112 ?M against MTB-H??Rv and 6.12 ?M against INHR-MTB, respectively.

SUBMITTER: Keng Yoon Y 

PROVIDER: S-EPMC3870127 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature