The 1,3-dipolar cycloaddition of deoxy-azido sugars 1 with O-benzylquercetin alkynes (5-7) to afford regioselective triazole-linked O-benzylquercetin glycoconjugates (8-10) was investigated in the presence of CuI/DIPEA in dichloromethane. All the developed glycoconjugates (8-10) were evaluated for anti-leishmanial activity against the promastigotes and amastigotes of Leishmania donovani. Graphical Abstract Click Inspired Synthesis of Antileishmanial Triazolyl O-Benzylquercetin Glycoconjugates.