In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II


Sonmez F., Bilen C. , Sumersan S., Gencer N., Isik S., Arslan O., ...More

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.29, no.1, pp.118-123, 2014 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 29 Issue: 1
  • Publication Date: 2014
  • Doi Number: 10.3109/14756366.2012.757222
  • Title of Journal : JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Page Numbers: pp.118-123
  • Keywords: Carbonic anhydrase, inhibition, saccharin, thiourea, urea, PARAOXONASE, DRUGS, PURIFICATION, SERUM

Abstract

In this study, in vitro inhibitory effects of some saccharin derivatives on purified carbonic anhydrase I and II were investigated using CO2 as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among the compounds, 6-(p-tolylthiourenyl) saccharin (6m) was found to be the most active one for hCA I activity (IC50 = 13.67 mu M) and 6-(m-methoxyphenylurenyl) saccharin (6b) was found to be the most active one for hCA II activity (IC50 = 6.54 mu M). Structure-activity relationships (SARs) study showed that, generally, thiourea derivatives (6l-v) inhibited more hCA I and hCA II than urea derivatives (6a-k). All compounds (excluding 6c and 6r) have higher inhibitory activity on hCA II than on hCA I.