Inhibition of mammalian carbonic anhydrase isoforms I, II and VI with thiamine and thiamine-like molecules

Here we determined the in vitro inhibitory effects of 5-(2-hydroxyethyl)-3,4-dimethylthiazolium iodide (1), 3-Benzyl-5-(2-hydroxyethyl)-4-methylthiazolium chloride (2) and thiamine (3) on human erythrocyte carbonic anhydrase I, II isozymes (hCA I and hCA II) and secreted isoenzyme CA VI. KI values r...

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Veröffentlicht in:Journal of enzyme inhibition and medicinal chemistry 2013-04, Vol.28 (2), p.316-319
Hauptverfasser: Özdemir, Zafer Ömer, entürk, Murat, Ekinci, Deniz
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Sprache:eng
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Zusammenfassung:Here we determined the in vitro inhibitory effects of 5-(2-hydroxyethyl)-3,4-dimethylthiazolium iodide (1), 3-Benzyl-5-(2-hydroxyethyl)-4-methylthiazolium chloride (2) and thiamine (3) on human erythrocyte carbonic anhydrase I, II isozymes (hCA I and hCA II) and secreted isoenzyme CA VI. KI values ranged from 0.38 to 2.27 µM for hCA I, 0.085 to 0.784 µM for hCA II and 0.062 to 0.593 µM for hCA VI, respectively. The compounds displayed relatively strong actions on hCA II, in the same range as the clinically used sulfonamidesethoxzolamide, zonisamide and acetazolamide.
ISSN:1475-6366
1475-6374
DOI:10.3109/14756366.2011.637200