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Molecules 2012, 17(2), 2248-2258; doi:10.3390/molecules17022248
Article

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

1,2,†, 2,†, 2, 2, 2, 3, 2,* , 1,*  and 2
1 Key Laboratory of Drug Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China 2 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, Sichuan, China 3 Department of Pharmaceutical and Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu 610065, Sichuan, China These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
Received: 3 February 2012 / Revised: 20 February 2012 / Accepted: 20 February 2012 / Published: 22 February 2012
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide; antitubercular; H37Rv; rifampin-resistant; affordable 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide; antitubercular; H37Rv; rifampin-resistant; affordable
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.

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MDPI and ACS Style

Ang, W.; Lin, Y.-N.; Yang, T.; Yang, J.-Z.; Pi, W.-Y.; Yang, Y.-H.; Luo, Y.-F.; Deng, Y.; Wei, Y.-Q. Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents. Molecules 2012, 17, 2248-2258.

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