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  • Title: Synthesis, in vitro evaluation, and molecular docking studies of novel hydrazineylideneindolinone linked to phenoxymethyl-1,2,3-triazole derivatives as potential α-glucosidase inhibitors.
    Author: Shareghi-Boroujeni D, Iraji A, Mojtabavi S, Faramarzi MA, Akbarzadeh T, Saeedi M.
    Journal: Bioorg Chem; 2021 Jun; 111():104869. PubMed ID: 33839583.
    Abstract:
    In this work, a novel series of hydrazineylideneindolinone linked to phenoxymethyl-1,2,3-triazole derivatives were designed, synthesized, and evaluated for their anti-α-glucosidase activity due to an urgent need to develop effective anti-diabetic agents. Among tested 15 compounds, 8 derivatives (9a, 9b, 9c, 9d, 9e, 9f, 9h, and 9o) demonstrated superior potency compared to that of positive control, acarbose. Particularly, compound 9d possessed the best anti-α-glucosidase activity with around a 46-fold improvement in the inhibitory activity. Additionally, 9d showed a competitive type of inhibition in the kinetic study and the molecular docking study demonstrated that it well occupied the binding pocket of the catalytic center through desired interactions with residues, correlating to the experimental results.
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