Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents

The synthesis and SAR profile of N-alkyl and heterocycle substituted 1,3-benzothiazin-4-one (BTZ) derivatives are described. The most potent compound 8o exhibits a MIC of 0.0001 μM against Mycobacterium tuberculosis H37Rv, 20-fold more potent than BTZ043 racemate.