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  • Title: Design, synthesis, in vitro, and in silico anti-α-glucosidase assays of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives as new anti-diabetic agents.
    Author: Sayahi MH, Zareei S, Halimi M, Alikhani M, Moazzam A, Mohammadi-Khanaposhtani M, Mojtabavi S, Faramarzi MA, Rastegar H, Taslimi P, Ibrahim EH, Ghramh HA, Larijani B, Mahdavi M.
    Journal: Sci Rep; 2024 Jul 09; 14(1):15791. PubMed ID: 38982268.
    Abstract:
    In this work, a novel series of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives 5a-n were designed by consideration of the potent α-glucosidase inhibitors containing indole and carboxamide-1,2,3-triazole-N-phenylacetamide moieties. These compounds were synthesized by click reaction and evaluated against yeast α-glucosidase. All the newly title compounds demonstrated superior potency when compared with acarbose as a standard inhibitor. Particularly, compound 5k possessed the best inhibitory activity against α-glucosidase with around a 28-fold improvement in the inhibition effect in comparison standard inhibitor. This compound showed a competitive type of inhibition in the kinetics. The molecular docking and dynamics demonstrated that compound 5k with a favorable binding energy well occupied the active site of α-glucosidase.
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