title: 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 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.
authors.affiliation: Institute for Research in Molecular Medicine, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
authors.forename: Yeong
authors.initials: Y
authors.lastname: Keng Yoon
authors.affiliation: 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.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Ashraf Ali
authors.affiliation: Institute for Research in Molecular Medicine, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
authors.forename: Tan Soo
authors.initials: TS
authors.lastname: Choon
authors.affiliation: Centre of Excellence for Research in AIDS (CERiA), University of Malaya, 50603 Kuala Lumpur, Malaysia.
authors.forename: Rusli
authors.initials: R
authors.lastname: Ismail
authors.affiliation: Institute for Research in Molecular Medicine, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
authors.forename: Ang
authors.initials: A
authors.lastname: Chee Wei
authors.affiliation: 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.
authors.forename: Raju
authors.initials: R
authors.lastname: Suresh Kumar
authors.affiliation: School of Chemical Science, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
authors.forename: Hasnah
authors.initials: H
authors.lastname: Osman
authors.affiliation: New Drug Discovery Research, Department of Medicinal Chemistry, Sunrise University, Alwar, Rajasthan 301030, India.
authors.forename: Farzana
authors.initials: F
authors.lastname: Beevi
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D006801:Humans; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D009579:Nitrobenzoates / Q000138:chemical synthesis / Q000737:chemistry; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy* / Q000382:microbiology / Q000473:pathology
chemical_list: D000995:Antitubercular Agents; D001562:Benzimidazoles; D009579:Nitrobenzoates; C081549:4-fluoro-3-nitrobenzoic acid; C031000:benzimidazole