Design, synthesis, and antitubercular activity of 3‐amidophenols with 5‐heteroatomic substitutions
作者： Niu‐niu Zhang , Yun‐xiang Tang , Lu Qian , Ya‐min Gao , Zhi‐yong Liu
关键词: Tuberculosis 、 Bacteria 、 Mycobacterium tuberculosis 、 Chemistry 、 Microbiology 、 Design synthesis
摘要: A series of novel 3-amidophenols with 5-heteroatomic substitutions were designed and synthesized. Several compounds showed potent antitubercular activity against Mycobacterium tuberculosis H37Ra (MIC = 0.25-5 μg/mL). Compounds 12j 14i also displayed good inhibitory M. H37Rv two clinically isolated multidrug-resistant strains (MIC = 0.39-3.12 μg/mL). The privileged compound certain oral efficacy on a mouse infection model. are non-cytotoxic L-O2 hepatocytes RAW264.7 macrophagocytes. They did not exert representative Gram-positive Gram-negative bacteria.
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