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
oleh: Mohammad Hossein Sayahi, Samira Zareei, Mohammad Halimi, Majid Alikhani, Ali Moazzam, Maryam Mohammadi-Khanaposhtani, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Hossein Rastegar, Parham Taslimi, Essam H. Ibrahim, Hamed A. Ghramh, Bagher Larijani, Mohammad Mahdavi
| Format: | Article |
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| Diterbitkan: | Nature Portfolio 2024-07-01 |
Deskripsi
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.