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Synthesis, In Vitro α-Amylase Inhibition Activity and Molecular Docking of some Coumarin Derivatives

  • Emna Chaabouni,
  • Ines Dhouib,
  • Emna Khdhiri,
  • Souhir Abid,
  • Noureddine Allouche,
  • Houcine Ammar,
  • Bassem Khemakhem

摘要

Coumarins represent a large number of natural and synthetic bioactive molecules. Their oxygen-containing heterocyclic structure makes them interesting in the field of medicinal chemistry. In this study, four coumarin derivatives (1b, 2b, 1c, and 3c) were synthesized and characterized by IR, 1H NMR, 13C NMR and elemental analysis. Additionally, the synthesized coumarins were investigated for their anti-diabetic potential. The results demonstrated that compound 1b displayed higher potency to inhibit α-amylase, with an IC90 value of 36 ± 1.04 µg/mL, than compound 3c with an IC90 value of 50 ± 1.15 µg/mL and compound 1c with an IC90 value of 66 ± 3.06 µg/mL. Our findings have been validated by molecular docking experiments. Thus, compound 1b would be used as an anti-postprandial hyperglycemia drug.

Graphical Abstract