Cu-Mediated Click Chemistry Approach: Synthesis, Characterization, and Anti-Mycobacterial Activity of 2-(4-((5-Bromo-3-formyl-1H-indol-1-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide Derivatives

This study presents the synthesis and optimization of series of 2-(4-((5-bromo-3-formyl-1H-indol-1-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide derivatives (8a-8t), synthesized through a multi-step process using a click chemistry approach in a mixed solvent system of tert-butanol, DMF, and water, catalyzed by copper. Optimal reaction conditions provide the highest yield. Subsequent vitro evaluation of 20 synthesized compounds for anti-mycobacterial activity against Mycobacterium tuberculosis revealed that most derivatives were ineffective due to solubility issues. Only a few compounds showed moderate activity, with the reference drug Rifampicin demonstrating significantly higher efficacy. This underscores the need for further optimization of these derivatives to improve their biological activity.