SYNTHESIS AND Α-GLUCOSIDASE INHIBITION OF DICLOROPHENYLINDOL-2-ONE DERIVATIVES

  • Đặng Thái Hoàng
  • , Nguyễn Văn Giang
  • Nguyễn Văn Giang
  • Nguyễn Văn An
  • Nguyễn Thu Huyền
  • Phạm Hải Long
  • Nguyễn Thị Sơn
  • Đỗ Huy Hoàng
Keywords: oxindole, indol-2-one, α-glucosidase inhibitor, molecular docking

Abstract

Oxindole (indol-2-one) is a crucial scaffold in medicinal chemistry for very common commercial drugs.
In our work, two oxindole derivatives have been synthesized, and confirmed by 1H & 13C-NMR, IR and
MS data. Compound 2 and 3 showed potent inhibitory activity against α-glucosidase with IC50 values of
57.5 and 348.7 μM, respectively. Molecular docking has been studied for the binding interactions of
these compounds with the active sites of the enzyme. Moreover, parameters drug-likeness and ADME
properties were calculated

điểm /   đánh giá
Published
2023-04-07