() type II NADH dehydrogenase (NDH-2) transports electrons into the mycobacterial respiratory pathway at the cost of reduction of NADH to NAD and is an attractive drug target. Herein, we have synthesised a series of 2-mercaptobenzothiazoles (C1-C14) and evaluated their anti-tubercular potential as NDH-2 inhibitors. The synthesised compounds C1-C14 were evaluated for MIC and ATP depletion against H37Ra, , and H37Rv mc 6230. Compounds C3, C4, and C11 were found to be the active molecules in the series and were further evaluated for their MIC against -resistant strains and for their bactericidal potential against H37Rv mc6230. The Peredox-mCherry-expressing strain was used to examine whether C3, C4, and C11 possess NDH-2 inhibitory potential. Furthermore, cytotoxicity analysis against HepG2 displayed a safety index (SI) of >10 for C3 and C4. To get an insight into the mode of interaction at NDH-2, we have performed computational analysis of our active compounds.
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| http://dx.doi.org/10.1039/d4md00118d | DOI Listing |
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