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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
Received: 3 February 2012; in revised form: 20 February 2012 / Accepted: 20 February 2012 / Published: 22 February 2012
(This article belongs to the Section Medicinal Chemistry)
Download PDF [285 KB, uploaded 18 June 2014]
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.

AMA 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(2):2248-2258.

Chicago/Turabian Style

Ang, Wei; Lin, Yan-Ni; Yang, Tao; Yang, Jian-Zhong; Pi, Wei-Yi; Yang, Ying-Hong; Luo, You-Fu; Deng, Yong; Wei, Yu-Quan. 2012. "Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents." Molecules 17, no. 2: 2248-2258.


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