Design, synthesis and evaluation of thiazole based amides for their antitubercular and PknG inhibitory activity

Abstract

A series of thiazole based amides have been designed and synthesized by solution-phase amide coupling of 2-aminothiazole and its derivatives with naturally occurring aromatic and heteroaromatic acids in excellent yield via DIC/HOBt protocol All the compounds have been evaluated for their antitubercular activity against M. tuberculosis virulent strain M. tuberculosis H37Rv and PknG inhibitory activity in the presence and absence of the inhibitors The compounds display moderate to significant PknG inhibitory activity (9.1-15.6% inhibition at 100 µM) as compared to the standard inhibitors and very moderate in vitro antitubercular activities against M. tuberculosis virulent strain M. tuberculosis H37Rv.