Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents
作者： Niu-niu Zhang , Zhi-yong Liu , Jie Liang , Yun-xiang Tang , Lu Qian
DOI: 10.1039/C8MD00212F
关键词: Biological evaluation 、 Cell culture 、 Chemistry 、 Tuberculosis 、 Bacteria 、 In vitro 、 Cytotoxicity 、 Design synthesis 、 Microbiology 、 Active compound
摘要: A series of m-amidophenol derivatives (6a-6l, 7a-7q, 9a, 9b, 12a-12c, 14 and 15) were designed synthesized. Their antitubercular activities evaluated in vitro against M. tuberculosis strains H37Ra H37Rv clinically isolated multidrug-resistant strains. Ten compounds displayed minimal inhibitory concentrations (MICs) below 2.5 μg mL-1 6g was the most active compound (MIC = 0.625 mL-1). Compounds 7a also showed potent activity 0.39 mL-1) several 0.39-3.125 The did not show normal Gram-positive Gram-negative bacteria. They exhibited low cytotoxicity HepG2 RAW264.7 cell lines. results demonstrated as an attractive scaffold for development new agents.
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