Synthesis and evaluation of alpha-glucosidase and pancreatic lipase inhibition by quinazolinone-coumarin hybrids


Mentese E., Karaali N., Akyuz G., Yilmaz F., Ulker S., KAHVECİ B.

CHEMISTRY OF HETEROCYCLIC COMPOUNDS, cilt.52, ss.1017-1024, 2016 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 52 Konu: 12
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1007/s10593-017-2002-3
  • Dergi Adı: CHEMISTRY OF HETEROCYCLIC COMPOUNDS
  • Sayfa Sayıları: ss.1017-1024

Özet

A new series of 2-substituted quinazolin-4(3H)-one derivatives including coumarin nucleus has been synthesized and screened for their lipase and a-glucosidase inhibition properties. Among the synthesized compounds, N'-{2-[2-(3,4-dichlorobenzyl)-4-oxoquinazolin-3(4H)-yl]acetyl}-2-oxo-2H-chromene-3-carbohydrazide and N'-{2-[2-(4-bromobenzyl)-4-oxoquinazolin-3(4H)-yl] acetyl}-2-oxo-2H-chromene-3-carbohydrazide showed the best inhibitory effect against a-glucosidase with IC50 values of 6.11 +/- 0.40 and 7.34 +/- 0.37 mu M, respectively. These compounds also showed strong anti-lipase activity (IC50 3.52 +/- 0.49 and 2.85 +/- 0.27 mu M, respectively).