Abstract
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. K(I) 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.
MeSH terms
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Carbonic Anhydrase Inhibitors / chemical synthesis
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Carbonic Anhydrase Inhibitors / chemistry
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Carbonic Anhydrase Inhibitors / pharmacology*
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Carbonic Anhydrases / isolation & purification
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Carbonic Anhydrases / metabolism*
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Dose-Response Relationship, Drug
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Erythrocytes / enzymology
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Humans
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Molecular Structure
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Protein Isoforms / antagonists & inhibitors
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Protein Isoforms / isolation & purification
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Protein Isoforms / metabolism
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Structure-Activity Relationship
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Thiamine / analogs & derivatives
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Thiamine / chemistry
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Thiamine / pharmacology*
Substances
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Carbonic Anhydrase Inhibitors
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Protein Isoforms
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Carbonic Anhydrases
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Thiamine