Synthesis and carbonic anhydrase inhibitory properties of novel coumarin derivatives


KARATAŞ M. O., ALICI B., Cakir U., Cetinkaya E., DEMİR D., Ergün A., ...More

Journal of Enzyme Inhibition and Medicinal Chemistry, vol.28, no.2, pp.299-304, 2013 (SCI-Expanded, Scopus)

  • Publication Type: Article / Article
  • Volume: 28 Issue: 2
  • Publication Date: 2013
  • Doi Number: 10.3109/14756366.2012.677838
  • Journal Name: Journal of Enzyme Inhibition and Medicinal Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.299-304
  • Keywords: Benzimidazolium, Carbonic anhydrase, Coumarin, Inhibition
  • Isparta University of Applied Sciences Affiliated: No

Abstract

A newly series of water-soluble 1-alkyl-3-(4-methyl-7, 8-dihydroxy-2H-chromen-2-one) benzimidazolium chloride salts (3a-j) were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II from human erythrocytes were purified by a simple one step procedure by using Sepharose 4B-L-tyrosine-sulphanilamide affinity column. The result showed that all the synthesized compounds were inhibited the CA isoenzymes activity. Among them, 3g and 3j were found to be most active (IC50 = 22.09 μM and 20.33 μM) for hCA I and hCA II, respectively.