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 (IC 50 = 15.1 μg/ml), 6d (IC 50 = 14.6 μg/ml) and 6e (IC 50 = 14.3 μg/ml) displayed potent antileishmanial activity when compared with standard sodium stibogluconate (IC 50 = 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.

Synthesis of diarylmethanes, a key building block for SGLT2 inhibitors, has been developed through ketone synthesis by Friedel–Crafts acylation with TiCl4, followed by reduction with TiCl4/NaBH4. The new protocol proceeded more cleanly than the previous methods employing AlCl3 and BF3·OEt2/Et3SiH to provide the diarylmethanes corresponding to canagliflozin, empagliflozin, and luseogliflozin in a highly expedient and affordable manner. In the case of a diarylmethane for the synthesis of dapagliflozin, the reduction step took place by an alternative method using InCl3/Al/BF3·OEt2.