论文题目：Identification of benzothiazinones containing 2-benzyl-2,7-diazaspiro[3.5]nonane moieties as new antitubercular agents

作者：Apeng Wang, Chao Ma, Yun Chai, Xiujun Liu, Kai Lv, Lei Fu, Bin Wang, Xuedong Jia, Mingliang Liu, Yu Lu

期刊名称：Eur J Med Chem

IF：5.572

年份：2020

卷期页：200:112409

A series of new benzothiazinone derivatives containing a symmetric 2-benzyl-2,7-diazaspiro[3.5]nonane moiety, based on the structure of LK02 discovered in our lab, were designed and synthesized. With one exception 3, all of them show excellent in vitro activity against both drug-sensitive and clinically isolated multidrug-resistant Mycobacterium tuberculosis (MTB) strains (MIC: < 0.016 μg/mL). Compound 2d with a methyl group at the benzylic carbon, was identified to have good safety and significant efficacy in an acute mouse model of TB, as well as better PK profiles than PBTZ169.