Tuberculosis (TB) is of increasing concern due to the recent emergence and spread of MDR-TB, XDR-TB,
TDR-TB and HIV/AIDS pandemic. There is urgent need for novel antitubercular agents which can shorten the treatment
duration. Based on isosteric replacement and 3D structural similarity between Linezolid, an oxazolidine antimycobacterial
agent, we have designed novel 4-amino-3,5-di(substituted)thiazolin-2(3H)thione/ones, synthesized and evaluated for their
antimycobacterial activity on Mycobacterium tuberculosis H37Rv strain. Some of the compounds exhibited potent antimycobacterial
activity with MIC values in the range of 1-2 µg/mL. Active compounds were further screened against
MDR-TB and XDR-TB strain and found to exhibit promising in vitro activity.
Keywords: Antimycobacterial activity, MDR-TB, thiazolin-thione/ones, XDR-TB.
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