Carbonic anhydrase inhibitory properties of some uracil derivatives

Turkoglu E. A., ŞENTÜRK M., Supuran C. T., EKİNCİ D.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.32, no.1, pp.74-77, 2017 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 32 Issue: 1
  • Publication Date: 2017
  • Doi Number: 10.1080/14756366.2016.1235043
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.74-77
  • Keywords: Carbonic anhydrase, hydroxyl, inhibitor, uracil derivatives, ISOZYMES I, ISOFORMS I, ENZYME, PURIFICATION, ANTITUMOR, TISSUE, VI
  • Ondokuz Mayıs University Affiliated: Yes

Abstract

Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4-12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The K-I values of the compounds 4-12 are in the range of 0.085-428 mu M for hCA I and of 0.1715-645 mu M against hCA II, respectively. It is concluded from the kinetic investigations, all compounds used in the study act as competitive inhibitors with substrate, 4-NPA. Uracil derivatives are emerging agents for the inhibiton of carbonic anhydrase which could be used in biomedicine.