IN VITRO INHIBITION OF PURIFIED HUMAN CARBONIC ANHYDRASE I AND II BY NOVEL FLUORENE DERIVATIVES


Demirhan H., Arslan M., KAYA M. O. , KAYA M. O. , Gencer N., Arslan O.

MACEDONIAN JOURNAL OF CHEMISTRY AND CHEMICAL ENGINEERING, vol.33, no.2, 2014 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 33 Issue: 2
  • Publication Date: 2014
  • Doi Number: 10.20450/mjcce.2014.440
  • Title of Journal : MACEDONIAN JOURNAL OF CHEMISTRY AND CHEMICAL ENGINEERING

Abstract

In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosine-sulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC50 = 21.4 mu M) for inhibition of hCA I and 5s was the most active (IC50 = 25.3 mu M) for inhibition of hCA II.