New phthalimide-benzamide-1,2,3-triazole hybrids; design, synthesis, alpha-glucosidase inhibition assay, and docking study

A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a-k as alpha-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds 8a-k against yeast alpha-glucosidase demonstrated that all they have excellent inhibitory activity in comparison with standard inhibitor acarbose. Among them, the most potent compound was compound 8d with inhibitory activity 18.5-fold more than acarbose. Kinetic study revealed that alpha-glucosidase inhibition of compound 8d was the competitive type. Furthermore, docking study suggested that compound 8d is more stable than acarbose in the active site of alpha-glucosidase.