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

dc.contributor.authorLv, Kai
dc.contributor.authorTao, Zeyu
dc.contributor.authorLiu, Qian
dc.contributor.authorYang, Lu
dc.contributor.authorWang, Bin
dc.contributor.authorWu, Shuo
dc.contributor.authorWang, Apeng
dc.contributor.authorHuang, Menghao
dc.contributor.authorLiu, Mingliang
dc.contributor.authorLu, Yu
dc.contributor.departmentMedicine, School of Medicineen_US
dc.date.accessioned2018-04-20T17:39:35Z
dc.date.available2018-04-20T17:39:35Z
dc.date.issued2018-05
dc.description.abstractWe 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.en_US
dc.eprint.versionAuthor's manuscripten_US
dc.identifier.citationLv, 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.2018.03.060en_US
dc.identifier.urihttps://hdl.handle.net/1805/15884
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.isversionof10.1016/j.ejmech.2018.03.060en_US
dc.relation.journalEuropean Journal of Medicinal Chemistryen_US
dc.rightsPublisher Policyen_US
dc.sourceAuthoren_US
dc.subjectbenzothiaziononesen_US
dc.subjectPBTZ169en_US
dc.subjectantimycobacterial activityen_US
dc.titleDesign, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moietyen_US
dc.typeArticleen_US
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