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Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents

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Author(s): Wei Ang | Yan-Ni Lin | Tao Yang | Jian-Zhong Yang | Wei-Yi Pi | Ying-Hong Yang | You-Fu Luo | Yong Deng | Yu-Quan Wei

Journal: Molecules
ISSN 1420-3049

Volume: 17;
Issue: 2;
Start page: 2248;
Date: 2012;
Original page

Keywords: 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide | antitubercular | H37Rv | rifampin-resistant | affordable

ABSTRACT
A novel series of 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide compounds were designed, synthesized and in vitro assessed for their antitubercular activities by a microdilution method. All the novel derivatives exerted potent or moderate active against M. tuberculosis H37Rv, with MIC values ranging from 4 to 64 μg/mL. The most potent derivative 3m showed an identical MIC value of 4 μg/mL for both M. tuberculosis H37Rv and rifampin-resistant M. tuberculosis 261. It demonstrated no inhibitory effects against six different tumor cell lines by a MTT assay and had a good safety profile in a vero cell line, providing a good lead for subsequent optimization in search of novel affordable antitubercular agents.

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