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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

Wei Ang ^1,2,† , Yan-Ni Lin ^2,† , Tao Yang ² , Jian-Zhong Yang ² , Wei-Yi Pi ² , Ying-Hong Yang ³ , You-Fu Luo ^2,* , Yong Deng ^1,*  and Yu-Quan Wei 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; in revised form: 20 February 2012 / Accepted: 20 February 2012 / Published: 22 February 2012

(This article belongs to the Section Medicinal Chemistry)

Download PDF Full-Text [285 KB, uploaded 22 February 2012 09:19 CET]

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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