Coumarin-Triazole-Thiazole hybrids: A new avenue in Antitubercular agents.

The present work reports the design and synthesis of a series of 2-(4-(((2-oxo-2H-chromen-4-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)-N-(thiazol-2-yl)acetamide derivatives (4a-4k), which were investigated for their potential against tubercular activities. The well-known click cycloaddition reaction of azido derivatives (3a-3k) and 4-(prop-2-yn-1-yloxy)-2H-chromen-2-one (2) in the presence of catalytic amount of CuSOin HO and DMF was employed. Notably, compounds 4c, 4d, and 4g showed the most promising results with MIC values against tuberculosis are 7.81 μg/mL, 2.61 μg/mL, and 7.81 μg/mL, respectively. Compounds (4a-4k) exhibited moderate to excellent antioxidant activities and low cytotoxicities. In addition, molecular docking studies were performed to investigate the binding interaction modes of the compounds (4a-4k) with various proteins and ligand sites.