Abstract
A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a–k as α-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds 8a–k against yeast α-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 α-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 α-glucosidase.
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Sadat-Ebrahimi, S.E., Rahmani, A., Mohammadi-Khanaposhtani, M. et al. New phthalimide-benzamide-1,2,3-triazole hybrids; design, synthesis, α-glucosidase inhibition assay, and docking study. Med Chem Res 29, 868–876 (2020). https://doi.org/10.1007/s00044-020-02522-7
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DOI: https://doi.org/10.1007/s00044-020-02522-7