I-A09

Description

I-A09 and its derivatives, specifically 1,2,3-triazole-adamantylacetamide hybrids 5aAAasAasAau , exhibit significant antitubercular activity. These hybrids were synthesized using copper-catalyzed click chemistry, combining bioactive fragments from antitubercular I-A09 and substituted adamantyl urea. The compound N- 1-adamantyl -2-azido acetamide was reacted with various alkyl/aryl acetylenes to produce new analogues. Among them, N- 1-adamantan-1-yl -2- 4- phenanthren-2-yl -1H-1,2,3-triazol-1-yl acetamide 5t showed the most promise with a minimum inhibitory concentration MIC of 3.12 ?g/mL against Mycobacterium tuberculosis H37Rv, and a selectivity index greater than 15.