受利福平/利福喷汀启发的新型苯并噻嗪酮的设计、合成及抗分枝杆菌活性
Design, synthesis and antimycobacterial activity of new benzothiazinones inspired by rifampicin/rifapentine.
作者信息
Wang Apeng, Lu Yu, Lv Kai, Ma Chao, Xu Shijie, Wang Bin, Wang Aoyu, Xia Guimin, Liu Mingliang
机构信息
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital College of Pharmacy, Medical University, Beijing 100149, China.
出版信息
Bioorg Chem. 2020 Sep;102:104135. doi: 10.1016/j.bioorg.2020.104135. Epub 2020 Jul 22.
A series of novel benzothiazinone derivatives containing a N-((methylene)amino)piperazine moiety, inspired by rifampicin/rifapentine, were designed and synthesized. Seven compounds 1a and 1e-j show excellent in vitro activity against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates (MIC: <0.029-0.110 μM), and accepted selective index (>1100->4000). Compound 1h displays good safety and pharmacokinetic profiles, suggesting its promising potential to be lead compound for future antitubercular drug discovery.
受利福平/利福喷汀启发，设计并合成了一系列含有N-((亚甲基)氨基)哌嗪部分的新型苯并噻嗪酮衍生物。七种化合物1a和1e-j对药物敏感的结核分枝杆菌菌株H37Rv和耐药临床分离株均表现出优异的体外活性（MIC：<0.029 - 0.110 μM），且选择性指数良好（>1100 -> 4000）。化合物1h显示出良好的安全性和药代动力学特征，表明其有潜力成为未来抗结核药物研发的先导化合物。
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