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<p>The review systematizes our studies over the past 10 years on the search for new synthetic α-amylase inhibitors obtained by diversity-oriented synthesis (DOS) based on multicomponent reactions of CH-acids with formaldehyde and <i>S</i>- or <i>N</i>-nucleophiles. The DOS strategy turned out to be a rational way to design sulfanylmethylazoles and oxazine derivatives of phenol and their metal complexes. Evaluation of the inhibitory activity of α-amylase <i>in vitro</i> and <i>in silico</i> showed that inhibition occurs by competitive, noncompetitive, and uncompetitive mechanisms, depending on the structure of these groups of compounds. Water-soluble complexes of palladium with a sulfanylmethylisoxazole ligand and copper with an aminomethylphenol ligand showed higher inhibitory activity against α-amylase than the reference drug acarbose.</p>

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Design and Antidiabetic Properties of Potential α-amylase Inhibitors (A Review)

  • 期刊论文

  • 发表日期：

    2026年2月1日

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  • V. R. Akhmetova,
  • N. S. Akhmadiev,
  • E. M. Galimova,
  • R. V. Kunakova

摘要

The review systematizes our studies over the past 10 years on the search for new synthetic α-amylase inhibitors obtained by diversity-oriented synthesis (DOS) based on multicomponent reactions of CH-acids with formaldehyde and S- or N-nucleophiles. The DOS strategy turned out to be a rational way to design sulfanylmethylazoles and oxazine derivatives of phenol and their metal complexes. Evaluation of the inhibitory activity of α-amylase in vitro and in silico showed that inhibition occurs by competitive, noncompetitive, and uncompetitive mechanisms, depending on the structure of these groups of compounds. Water-soluble complexes of palladium with a sulfanylmethylisoxazole ligand and copper with an aminomethylphenol ligand showed higher inhibitory activity against α-amylase than the reference drug acarbose.