Carbonic anhydrase inhibitory properties of some uracil derivatives

J Enzyme Inhib Med Chem. 2017 Dec;32(1):74-77. doi: 10.1080/14756366.2016.1235043.

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 KI values of the compounds 4-12 are in the range of 0.085-428 µM for hCA I and of 0.1715-645 µM 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.

Keywords: Carbonic anhydrase; hydroxyl; inhibitor; uracil derivatives.

MeSH terms

  • Carbonic Anhydrase Inhibitors / pharmacology*
  • Carbonic Anhydrases / blood
  • Carbonic Anhydrases / isolation & purification
  • Chromatography, Affinity
  • Erythrocytes / enzymology
  • Humans
  • Isoenzymes / blood
  • Isoenzymes / isolation & purification
  • Uracil / pharmacology*

Substances

  • Carbonic Anhydrase Inhibitors
  • Isoenzymes
  • Uracil
  • Carbonic Anhydrases