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Design, synthesis and antimycobacterial activity of new benzothiazinones inspired by rifampicin/rifapentine.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-07-22 , DOI: 10.1016/j.bioorg.2020.104135 Apeng Wang 1 , Yu Lu 2 , Kai Lv 1 , Chao Ma 1 , Shijie Xu 1 , Bin Wang 2 , Aoyu Wang 3 , Guimin Xia 1 , Mingliang Liu 1
中文翻译：
受利福平/利福喷丁启发的新型苯并噻嗪酮的设计，合成和抗分枝杆菌活性。
更新日期：2020-07-29
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-07-22 , DOI: 10.1016/j.bioorg.2020.104135 Apeng Wang 1 , Yu Lu 2 , Kai Lv 1 , Chao Ma 1 , Shijie Xu 1 , Bin Wang 2 , Aoyu Wang 3 , Guimin Xia 1 , Mingliang Liu 1
Affiliation
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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.
中文翻译：
受利福平/利福喷丁启发的新型苯并噻嗪酮的设计，合成和抗分枝杆菌活性。
在利福平/利福喷丁的启发下，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。七个化合物1a和1e - j对药物敏感性MTB株H37Rv和耐药性临床分离株（MIC：<0.029-0.110μM）均显示出优异的体外活性，并具有可接受的选择指数（> 1100-> 4000）。化合物1h显示出良好的安全性和药代动力学特征，表明其有望成为未来抗结核药物发现的先导化合物。
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