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., ...Daha Fazla

RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY, cilt.42, sa.5, ss.506-511, 2016 (SCI-Expanded, Scopus) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 42 Sayı: 5
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1134/s1068162016050046
  • Dergi Adı: RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.506-511
  • Anahtar Kelimeler: carbonic anhydrase, coumarin, inhibitor, structure-activity relationship, SELECTIVE INHIBITORS, COUMARINS, POTENT
  • Bezmiâlem Vakıf Üniversitesi Adresli: Evet

Özet

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.