Novel acyl hydrazide derivatives of polyhydroquinoline as potent anti-diabetic and anti-glycating agents: Synthesis, in vitro α-amylase, α-glucosidase inhibition and anti-glycating activity with molecular docking insights

Jun 12, 2024Bioorganic chemistry

New compounds based on polyhydroquinoline that may strongly block enzymes related to diabetes and prevent sugar damage: synthesis, enzyme tests, and computer modeling

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Abstract

Seven compounds exhibited notable α-amylase inhibitory activity with IC values ranging from 3.51 ± 2.13 to 11.92 ± 2.30 µM.

  • Six compounds demonstrated potent α-glucosidase inhibitory activity compared to the standard acarbose.
  • Eight derivatives showed excellent anti-glycating activity with IC values from 6.91 ± 2.66 to 15.80 ± 1.87 µM, outperforming the standard rutin.
  • Molecular docking analysis indicated strong interactions between most compounds and the enzymes α-amylase and α-glucosidase.
  • Compounds fit well into the binding pockets of α-amylase and α-glucosidase.
  • Compounds 2a and 2f were identified as the most potent based on docking scores against both enzymes.

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