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Antituberculosis: synthesis and antimycobacterial activity of novel benzimidazole derivatives

Keng Yoon Y 1 , Ashraf Ali M 2 , Choon TS 1 , Ismail R 3 , Chee Wei A 1 , Suresh Kumar R 4 Show all authors , Osman H 5 , Beevi F 6

Affiliations 

  • 1 Institute for Research in Molecular Medicine, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia
  • 2 Institute for Research in Molecular Medicine, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia ; New Drug Discovery Research, Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301030, India ; New Drug Discovery Research, Department of Medicinal Chemistry, Sunrise University, Alwar, Rajasthan 301030, India
  • 3 Centre of Excellence for Research in AIDS (CERiA), University of Malaya, 50603 Kuala Lumpur, Malaysia
  • 4 School of Chemical Science, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia ; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh, Saudi Arabia
  • 5 School of Chemical Science, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia
  • 6 New Drug Discovery Research, Department of Medicinal Chemistry, Sunrise University, Alwar, Rajasthan 301030, India
Biomed Res Int, 2013;2013:926309.
PMID: 24381946 DOI: 10.1155/2013/926309

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 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 (5 g) was found to be the most active with MIC of 0.112 μM against MTB-H₃₇Rv and 6.12 μM against INHR-MTB, respectively.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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