Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II

Kilicaslan S., Arslan M., Ruya Z., Bilen C., Ergun A., Gencer N., ...More

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.31, no.6, pp.1300-1305, 2016 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 31 Issue: 6
  • Publication Date: 2016
  • Doi Number: 10.3109/14756366.2015.1128426
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1300-1305
  • Keywords: Carbonic anhydrase, enzyme inhibitor, sulfonamide, thiazole, INHIBITORY PROPERTIES, CYANAMIDE HYDRATION, ESTERASE-ACTIVITIES, VITRO INHIBITION, DERIVATIVES, MECHANISM, ISOZYMES, COUMARINS, DRUGS
  • Yıldız Technical University Affiliated: No

Abstract

Sulfonamide-bearing thiazole compounds were synthesized 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 12 synthesized sulfonamide (5a-l) on the hydratase and esterase activities of these isoenzymes (hCA-I and hCA-II) were studied in vitro. In relation to these activities, the inhibition equilibrium constants (Ki) were determined. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. Among them 5b was found to be the most active (IC50 = 0.35 mu M; Ki: 0.33 mu M) for hCA I and hCA II.