Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives

doi:10.1155/2013/926309

Paper

Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives

Published Dec 5, 2013 · Yeong Keng Yoon, M. Ashraf Ali, T. S. Choon

BioMed Research International

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28

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

In Vitro Study

Study Snapshot

Novel benzimidazole derivatives show promising antituberculosis activity, with ethyl 1-(2-(4-(4-(ethoxycarbonyl)-2-aminophenyl)piperazin-1-yl)ethyl)-2-(4-

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Antituberculosis: Synthesis and Antimycobacterial Activity of Novel Benzimidazole Derivatives

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References

Supplementary Figure 2

CD8+ cells in the IEL and MLN are activated by CD3/CD28 stimulation, forming a distinct population from naive CD8+ cells.

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5-phenyl-3-isoxazolecarboxylic acid ethyl esters show potent, selective, and versatile anti-TB activity, offering potential for further TB drug development.

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Citations