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Synthesis of quinolinyl pyrazole analogues by ring functionalization as well as molecular hybridization strategy is adopted. Diverse functional groups were assembled around the privileged scaffold viz., 2-methyl-3-(1H-pyrazol-5-yl)quinoline. A series of quinolinyl pyrazole analogues with 1,4-disubstituted 1,2,3-triazole moiety, were synthesized employing Click reaction conditions. All 29 synthesized were evaluated for antitubercular activity against Mycobacterium smegmatis strain; wherein eight compounds were active and two promising. Compounds also exhibited the low cytotoxicity against A549 cell line.[a] Dr.