Antituberculosis: Synthesis and antimycobacterial activity of novel benzimidazole derivatives

Yeong Keng Yoon; Mohamed Ashraf Ali; Tan Soo Choon; Rusli Ismail; Ang Chee Wei; Raju Suresh Kumar; Hasnah Osman; Farzana Beevi

doi:10.1155/2013/926309

Antituberculosis: Synthesis and antimycobacterial activity of novel benzimidazole derivatives

Yeong Keng Yoon, Mohamed Ashraf Ali, Tan Soo Choon, Rusli Ismail, Ang Chee Wei, Raju Suresh Kumar, Hasnah Osman, Farzana Beevi

Research output: Contribution to journal › Article › Research › peer-review

23 Citations (Scopus)

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 Hv (MTB-Hv) 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 M. 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 M against MTB-Hv and 6.12 M against INHR-MTB, respectively.

Original language	English
Article number	926309
Journal	BioMed Research International
Volume	2013
DOIs	https://doi.org/10.1155/2013/926309
Publication status	Published - 2013
Externally published	Yes

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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 Hv (MTB-Hv) 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 M. 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 M against MTB-Hv and 6.12 M against INHR-MTB, respectively.",

author = "{Keng Yoon}, Yeong and {Ashraf Ali}, Mohamed and Choon, {Tan Soo} and Rusli Ismail and {Chee Wei}, Ang and {Suresh Kumar}, Raju and Hasnah Osman and Farzana Beevi",

year = "2013",

doi = "10.1155/2013/926309",

language = "English",

volume = "2013",

journal = "BioMed Research International",

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T1 - Antituberculosis

T2 - Synthesis and antimycobacterial activity of novel benzimidazole derivatives

AU - Keng Yoon, Yeong

AU - Ashraf Ali, Mohamed

AU - Choon, Tan Soo

AU - Ismail, Rusli

AU - Chee Wei, Ang

AU - Suresh Kumar, Raju

AU - Osman, Hasnah

AU - Beevi, Farzana

PY - 2013

Y1 - 2013

N2 - 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 Hv (MTB-Hv) 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 M. 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 M against MTB-Hv and 6.12 M against INHR-MTB, respectively.

AB - 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 Hv (MTB-Hv) 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 M. 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 M against MTB-Hv and 6.12 M against INHR-MTB, respectively.

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DO - 10.1155/2013/926309

M3 - Article

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VL - 2013

JO - BioMed Research International

JF - BioMed Research International

SN - 2314-6133

M1 - 926309

ER -

Antituberculosis: Synthesis and antimycobacterial activity of novel benzimidazole derivatives

Abstract

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