In vitro inhibition effects on erythrocyte carbonic anhydrase I and II and structure-activity relationships of cumarylthiazole derivatives


Kurt B. , Sonmez F., GÖKÇE B., Ergun A., Gencer N., Demir T., ...More

RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY, vol.42, no.5, pp.506-511, 2016 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 42 Issue: 5
  • Publication Date: 2016
  • Doi Number: 10.1134/s1068162016050046
  • Title of Journal : RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
  • Page Numbers: pp.506-511
  • Keywords: carbonic anhydrase, coumarin, inhibitor, structure-activity relationship, SELECTIVE INHIBITORS, COUMARINS, POTENT

Abstract

Coumarin and heterocyclic compounds incorporating urea have clinical applications as antiepileptics, diuretics, and antiglaucoma agents due to their carbonic anhydrase inhibitory properties. We investigated inhibition of carbonic anhydrase I and II with a series of coumarylthiazole derivatives containing urea/thiourea groups. All the investigated compounds exhibited inhibitory activity on both hCA I and hCA II, with 1-(3-chlorophenyl)-3-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)urea being the strongest inhibitor. Structure-activity relationship study showed that most of urea derivatives were more inhibiting for hCA I and hCA II than thiourea derivatives. The electron-withdrawing groups at the phenyl ring increased the inhibitory activity compared to electron-donating groups.