Journal of medicinal chemistryMicrobial Sensitivity TestsStructure-Activity RelationshipThiazinesDrug DesignAntitubercular Agents
Discovery, Design, and Synthesis of Novel 2-Benzyl-2,7-diazaspiro[3.5]nonane Benzothiazinones with Broad-Spectrum Antimycobacterial Activity.
Jizhou Wu, Chao Ma, Meng Wei, Xiuzhen Chen, Weixiao Wang, Jinghan Gao, Junjie Huang, Xiaorui Ji, Meijiao Wei, Mingliang Liu, Apeng Wang, Kai Lv, Wei Chen
Published: 202510.1021/acs.jmedchem.5c02429
Abstract
Despite their nanomolar potency against M. tuberculosis (MTB), benzothiazinone (BTZs) DprE1 inhibitors like PBTZ169 are ineffective against nontuberculous mycobacteria (NTM) due to a Cys387Ala mutation in the NTM DprE1 target. Here, 529 BTZs in our l…
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