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In the present work, we have synthesized novel quinoline‐conjugated 1,2,3‐triazole derivatives 6a–l starting from substituted acetanilides in five steps. The synthesized compounds were screened for their antileishmanial activity. Quinoline‐conjugated 1,2,3‐triazole compounds 6c (IC50 = 15.1 μg/ml), 6d (IC50 = 14.6 μg/ml) and 6e (IC50 = 14.3 μg/ml) displayed potent antileishmanial activity when compared with standard sodium stibogluconate (IC50 = 14.3 ± 1.5 μg/ml). A molecular docking study against Leishmania major pteridine reductase (Lm‐PTR1) suggests that these compounds have the potential to become lead molecules in antileishmanial drug discovery. [ABSTRACT FROM AUTHOR]