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

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Date
2018-05
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English
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Elsevier
Abstract

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 μg/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 μg/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.

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Lv, K., Tao, Z., Liu, Q., Yang, L., Wang, B., Wu, S., … Lu, Y. (2018). Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety. European Journal of Medicinal Chemistry, 151, 1–8. https://doi.org/10.1016/j.ejmech.2018.03.060
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European Journal of Medicinal Chemistry
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Article
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