Synthesis, biological evaluation and molecular docking studies of quinoline-conjugated 1,2,3-triazole derivatives as antileishmanial agents

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 mu g/ml), 6d (IC50 = 14.6 mu g/ml) and 6e (IC50 = 14.3 mu g/ml) displayed potent antileishmanial activity when compared with standard sodium stibogluconate (IC50 = 14.3 +/- 1.5 mu g/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.