In this section, you can access to the latest technical information related to the FUTURE project topic.

Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis

A series of novel benzothiazinone derivatives containing a N-(amino)piperazine moiety, based on the structure of WAP-1902 discovered in our lab, were designed and synthesized as new anti-TB agents. Many of the compounds exhibited excellent in?vitro activity against both drug-sensitive MTB strain H37Rv and multidrug-resistant clinical isolates (MIC: < 0.016??g/mL), and good safety index (CC50: >64??g/mL). Especially compound 1o displayed low hERG cardiac toxicity and acceptable oral pharmacokinetic profiles, indicating its promising potential to be a lead compound for future antitubercular drug discovery.

» Author: Apeng Wang, Shijie Xu, Yun Chai, Guimin Xia, Bin Wang, Kai Lv, Chao Ma, Dan Wang, Aoyu Wang, Xiaoyu Qin, Mingliang Liu, Yu Lu

» Publication Date: 05/06/2021

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