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

AbstractA new series of phthalimide-benzamide-1,2,3-triazole hybrids8a –k asα-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds8a –k against yeastα-glucosidase demonstrated that all they have excellent inhibitory activity in comparison with standard inhibitor acarbose. Among them, the most potent compound was compound8d with inhibitory activity 18.5-fold more than acarbose. Kinetic study revealed thatα-glucosidase inhibition of compound8d was the competitive type. Furthermore, docking study suggested that compound8d is more stable than acarbose in the active site ofα-glucosidase.

Source: Medicinal Chemistry Research - March 15, 2020 Category: Chemistry Source Type: research