Design and synthesis of novel xanthone-triazole derivatives as potential antidiabetic agents: α-Glucosidase inhibition and glucose uptake promotion

Jun 4, 2019European journal of medicinal chemistry

New xanthone-triazole compounds that may help diabetes by blocking sugar digestion and boosting glucose absorption

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Abstract

Compound 5e demonstrated an IC value of 2.06 μM, making it the most potent α-glucosidase inhibitor identified.

  • Most novel xanthone-triazole derivatives exhibited better α-glucosidase inhibitory activities than the parental compound and the positive control.
  • Compounds 5e, 5g, 5h, 6c, 6d, 6g, and 6h were found to be noncompetitive inhibitors of α-glucosidase.
  • Molecular docking studies indicated that these compounds bind to allosteric sites away from the active site.
  • Compounds 5e, 6a, 6c, and 7g significantly promoted glucose uptake in HepG2 cells.
  • Most compounds displayed low toxicity to the human normal hepatocyte cell line (LO2).

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