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

Molecules

Wei Ang¹  Yan-Ni Lin¹  Tao Yang¹  Jian-Zhong Yang¹  Wei-Yi Pi¹  Ying-Hong Yang¹  You-Fu Luo¹  Yong Deng¹ 

[1] ¹Key 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

关键词: 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide;    antitubercular;    H₃₇Rv;    rifampin-resistant;    affordable;   

DOI  :  10.3390/molecules17022248

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.