Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.

ABSTRACT: With growing concerns regarding target residue mutation hovering over established anti-TB pharmacophores, it is imperative to have reserve chemotypes at our disposal to curb unrestrained spread of tuberculosis. In this context, we herein present the synthesis and bio-evaluation of a library of new nitrobenzothiazinone (BTZ) congeners comprising 2-mercapto/amino-benzothiazinone tethered 1,2,3-triazole hybrids as antitubercular agents. In preliminary screening, 10 out of 37 compounds displayed substantial in vitro potency against Mtb H37Rv (MIC 0.5-8 μg mL^-1). Structural optimization of the initial hit 5o (MIC 0.5 μg mL^-1) led to identification of linker variants 9a, 9b, 9c, and 9d exhibiting potent anti-TB activity (MIC 0.03-0.12 μg mL^-1). When tested

SUBMITTER: Sahoo SK 

PROVIDER: S-EPMC9132192 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature