Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives

الملخص EN

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 H37Rv (MTB-H37Rv) 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 μM.

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 μM against MTB-H37Rv and 6.12 μM against INHR-MTB, respectively.