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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 Publisher Pubmed



Sayahi MH1 ; Zareei S2 ; Halimi M3 ; Alikhani M4 ; Moazzam A2 ; Mohammadikhanaposhtani M5 ; Mojtabavi S6 ; Faramarzi MA6 ; Rastegar H7 ; Taslimi P8 ; Ibrahim EH9, 10, 11 ; Ghramh HA9, 10, 12 ; Larijani B2 ; Mahdavi M2
Authors

Source: Scientific Reports Published:2024


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. © The Author(s) 2024.
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