In vitro inhibition effects on erythrocyte carbonic anhydrase I and II and structure-activity relationships of cumarylthiazole derivatives
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY, vol.42, no.5, pp.506-511, 2016 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 42 Issue: 5
- Publication Date: 2016
- Doi Number: 10.1134/s1068162016050046
- Journal Name: RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.506-511
- Süleyman Demirel University Affiliated: Yes
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.