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 Hv (MTB-Hv) 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 (5g) was found to be the most active with MIC of 0.112 M against MTB-Hv and 6.12 M against INHR-MTB, respectively. © 2013 Yeong Keng Yoon et al.