Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives

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(37)Rv (MTB-H(37)Rv) and INH-resista...

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Detalles Bibliográficos
Autores principales: Keng Yoon, Yeong, Ashraf Ali, Mohamed, Choon, Tan Soo, Ismail, Rusli, Chee Wei, Ang, Suresh Kumar, Raju, Osman, Hasnah, Beevi, Farzana
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2013
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3870127/
https://www.ncbi.nlm.nih.gov/pubmed/24381946
http://dx.doi.org/10.1155/2013/926309
Descripción
Sumario: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(37)Rv (MTB-H(37)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 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-H(37)Rv and 6.12 μM against INHR-MTB, respectively.

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