Diabetes mellitus (DM) is a metabolic condition that is a major health concern around the world. The current study investigates the synthesis of a series of chalcone and 1H-1,2,3-triazole hybrid compounds and their in vitro inhibitory potential against α-glucosidase. The antidiabetic analysis revealed that compounds 4a and 4b are highly active agents with IC50 of 3.90 and 4.77 µM, respectively. These results are close to quercetin (IC50 = 4.24 µM) as the reference standard. Molecular docking study strongly supports the active interaction of the 4a and 4b to the enzyme through cation-π interaction and hydrogen bonding between the ligands and the active site of Saccharomyces cerevisiae α-glucosidase enzyme. This study broadened the potential of designing chalcone-triazole hybrid compounds as antidiabetic drug candidates in the pharmaceutical sector.
Keywords: 1H-1,2,3-triazole; Saccharomyces cerevisiae α-glucosidase; antidiabetic; chalcone; hybrid compound.