Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety
dc.contributor.author | Lv, Kai | |
dc.contributor.author | Tao, Zeyu | |
dc.contributor.author | Liu, Qian | |
dc.contributor.author | Yang, Lu | |
dc.contributor.author | Wang, Bin | |
dc.contributor.author | Wu, Shuo | |
dc.contributor.author | Wang, Apeng | |
dc.contributor.author | Huang, Menghao | |
dc.contributor.author | Liu, Mingliang | |
dc.contributor.author | Lu, Yu | |
dc.contributor.department | Medicine, School of Medicine | en_US |
dc.date.accessioned | 2018-04-20T17:39:35Z | |
dc.date.available | 2018-04-20T17:39:35Z | |
dc.date.issued | 2018-05 | |
dc.description.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. | en_US |
dc.eprint.version | Author's manuscript | en_US |
dc.identifier.citation | 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 | en_US |
dc.identifier.uri | https://hdl.handle.net/1805/15884 | |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.relation.isversionof | 10.1016/j.ejmech.2018.03.060 | en_US |
dc.relation.journal | European Journal of Medicinal Chemistry | en_US |
dc.rights | Publisher Policy | en_US |
dc.source | Author | en_US |
dc.subject | benzothiazionones | en_US |
dc.subject | PBTZ169 | en_US |
dc.subject | antimycobacterial activity | en_US |
dc.title | Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety | en_US |
dc.type | Article | en_US |