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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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
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author Keng Yoon, Yeong
Ashraf Ali, Mohamed
Choon, Tan Soo
Ismail, Rusli
Chee Wei, Ang
Suresh Kumar, Raju
Osman, Hasnah
Beevi, Farzana
author_facet Keng Yoon, Yeong
Ashraf Ali, Mohamed
Choon, Tan Soo
Ismail, Rusli
Chee Wei, Ang
Suresh Kumar, Raju
Osman, Hasnah
Beevi, Farzana
author_sort Keng Yoon, Yeong
collection PubMed
description 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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spelling pubmed-38701272013-12-31 Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives Keng Yoon, Yeong Ashraf Ali, Mohamed Choon, Tan Soo Ismail, Rusli Chee Wei, Ang Suresh Kumar, Raju Osman, Hasnah Beevi, Farzana Biomed Res Int Research Article 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. Hindawi Publishing Corporation 2013 2013-12-05 /pmc/articles/PMC3870127/ /pubmed/24381946 http://dx.doi.org/10.1155/2013/926309 Text en Copyright © 2013 Yeong Keng Yoon et al. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Keng Yoon, Yeong
Ashraf Ali, Mohamed
Choon, Tan Soo
Ismail, Rusli
Chee Wei, Ang
Suresh Kumar, Raju
Osman, Hasnah
Beevi, Farzana
Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives
title Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives
title_full Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives
title_fullStr Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives
title_full_unstemmed Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives
title_short Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives
title_sort antituberculosis: synthesis and antimycobacterial activity of novel benzimidazole derivatives
topic Research Article
url 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
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