In vitro inhibition effects on erythrocyte carbonic anhydrase I and II and structure-activity relationships of cumarylthiazole derivatives |
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| Authors: | Belma Z. Kurt Fatih Sonmez Basak Gokce Adem Ergun Nahit Gencer Taki Demir Oktay Arslan Mustafa Kucukislamoglu |
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| Affiliation: | 1.Deparment of Medicinal Chemistry, Faculty of Pharmacy,Bezmialem Vakif University,Istanbul,Turkey;2.Pamukova Vocational High School,Sakarya University,Sakarya,Turkey;3.Faculty of Pharmacy,Suleyman Demirel University,Isparta,Turkey;4.Department of Chemistry, Faculty of Art and Sciences,Balikesir University,Balikesir,Turkey;5.Department of Chemistry, Faculty of Arts and Science,Sakarya University,Sakarya,Turkey |
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| 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. |
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