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

Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety

We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC?<?1??g/mL) against drug-susceptible Mycobacterium tuberculosis H37RV strain. After two set of modifications, compound 2i were found to display comparable in vitro anti-TB activity (MIC?<?0.016??g/mL) to PBTZ169 against drug-sensitive and resistant mycobacterium tuberculosis strains. Compound 2i also showed acceptable PK profiles. Studies to determine PK profiles in lung and in vivo efficacy of 2i are currently under way.

» Author: Kai Lv, Zeyu Tao, Qian Liu, Lu Yang, Bin Wang, Shuo Wu, Apeng Wang, Menghao Huang, Mingliang Liu, Yu Lu

» Reference: European Journal of Medicinal Chemistry, Volume 151

» Publication Date: 10/05/2018

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