Synthesis and carbonic anhydrase inhibitory properties of new spiroindoline-substituted sulphonamide compounds

Gulec O., Arslan M., Gencer N., Ergun A., Bilen C., Arslan O.

ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY, cilt.123, sa.5, ss.306-312, 2017 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 123 Sayı: 5
  • Basım Tarihi: 2017
  • Doi Numarası: 10.1080/13813455.2017.1332651
  • Dergi Adı: ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.306-312
  • Yıldız Teknik Üniversitesi Adresli: Hayır

Özet

New spiroindoline-substituted sulphonamide compounds were synthesised and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of the 14 synthesised sulphonamides (6a-n) on esterase activities of these isoenzymes were studied in vitro. In relation to these activities, the inhibition equilibrium constants (K-i) were determined. The results showed that all the synthesised compounds inhibited the carbonic anhydrase (CA) isoenzyme activity. Among them, 6b was found to be the most active (K-i: 0.042 mu M) for hCA I and 6a (K-i: 0.151 mu M) for hCA II.