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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.

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.

SUBMITTER: Sayahi MH 

PROVIDER: S-EPMC11233587 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature

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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.

Sayahi Mohammad Hossein MH   Zareei Samira S   Halimi Mohammad M   Alikhani Majid M   Moazzam Ali A   Mohammadi-Khanaposhtani Maryam M   Mojtabavi Somayeh S   Faramarzi Mohammad Ali MA   Rastegar Hossein H   Taslimi Parham P   Ibrahim Essam H EH   Ghramh Hamed A HA   Larijani Bagher B   Mahdavi Mohammad M  

Scientific reports 20240709 1

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 bes  ...[more]

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