Discovery of meta-Amido Bromophenols as New Antitubercular Agents

Jie Liang; Yun-xiang Tang; Xiang-zheng Tang; Hua-ju Liang; Yamin Gao; Cuiting Fang; Tian-yu Zhang; Ming Yan

doi:10.1248/cpb.c18-00917

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Discovery of meta-Amido Bromophenols as New Antitubercular Agents

Jie Liang, Yun-xiang Tang, Xiang-zheng Tang, Hua-ju Liang, Yamin Gao, Cuiting Fang, Tian-yu Zhang, Ming Yan

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Jie Liang
School of Pharmaceutical Sciences, Sun Yat-sen University
Yun-xiang Tang
State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science
Institute of Physical Science and Information Technology, Anhui University
Xiang-zheng Tang
School of Pharmaceutical Sciences, Sun Yat-sen University
Hua-ju Liang
School of Pharmaceutical Sciences, Sun Yat-sen University
Yamin Gao
State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science
University of Chinese Academy of Sciences (UCAS)
Cuiting Fang
State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science
University of Chinese Academy of Sciences (UCAS)
Tian-yu Zhang
State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science
University of Chinese Academy of Sciences (UCAS)
Ming Yan Corresponding author
School of Pharmaceutical Sciences, Sun Yat-sen University

Keywords: Mycobacterium tuberculosis, meta-amido bromophenol, antitubercular agent

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Supplementary material

2019 Volume 67 Issue 4 Pages 372-381

DOI https://doi.org/10.1248/cpb.c18-00917

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Abstract

A series of meta-amido bromophenol derivatives were designed and synthesized. The compounds were found to potently inhibit the growth of Mycobacterium tuberculosis H37Ra. They also exhibited moderate inhibitory activity against Mycobacterium tuberculosis H37Rv and multidrug-resistant strains. The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. Moderate cytotoxicities and good metabolic stability were observed for the selected compounds. The results demonstrated meta-amido bromophenols as a new class of antitubercular agents with good potentials.

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