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 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; in revised form: 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

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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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