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, vol.52, no.12, pp.1017-1024, 2016 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 52 Issue: 12
  • Publication Date: 2016
  • Doi Number: 10.1007/s10593-017-2002-3
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1017-1024
  • Keywords: coumarins, quinazolin-4(3H)-one, anti-lipase activity, alpha-glucosidase inhibition, microwave, ultrasonication, DERIVATIVES, POTENT, AGENTS, ANTIBACTERIAL, ANTIOXIDANTS, ALKALOIDS, ORLISTAT, SERIES, DRUG, MICE
  • Recep Tayyip Erdoğan University Affiliated: Yes


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).