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

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

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 (CC BY 3.0).

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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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