Synthesis, in vitro evaluation, and molecular docking studies of novel hydrazineylideneindolinone linked to phenoxymethyl-1,2,3-triazole derivatives as potential α-glucosidase inhibitors.
作者： Aida Iraji , Tahmineh Akbarzadeh , Mina Saeedi , Mohammad Ali Faramarzi , Somayeh Mojtabavi
DOI: 10.1016/J.BIOORG.2021.104869
关键词:
摘要: 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 an urgent need develop effective anti-diabetic agents. Among tested 15 compounds, 8 (9a, 9b, 9c, 9d, 9e, 9f, 9h, 9o) demonstrated superior potency compared that positive control, acarbose. Particularly, compound 9d possessed the best with around 46-fold improvement in inhibitory activity. Additionally, showed competitive type inhibition kinetic study molecular docking it well occupied binding pocket catalytic center through desired interactions residues, correlating experimental results.
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