Synthesis and carbonic anhydrase inhibitory properties of novel coumarin derivatives

Makaleler > Tam Makale · 2012

Yazarlar: Mert Olgun Karatas, Bülent Alici, Umit Cakir, Engin Cetinkaya, Dudu Demir, Adem Ergün, Nahit Gençer, Oktay Arslan

Journal of Enzyme Inhibition and Medicinal Chemistry, Uluslararası, Wos, 2012, cilt 28, ss 299-304

DOI: 10.3109/14756366.2012.677838

Özet

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 (IC(50) = 22.09 µM and 20.33 µM) for hCA I and hCA II, respectively.

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