Department of Chemistry, Art and Science Faculty, Kirklareli University, Kirklareli, Turkey.
J Enzyme Inhib Med Chem. 2013 Apr;28(2):316-9. doi: 10.3109/14756366.2011.637200. Epub 2011 Dec 6.
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.
在这里,我们测定了 5-(2-羟乙基)-3,4-二甲基噻唑鎓碘化物(1)、3-苄基-5-(2-羟乙基)-4-甲基噻唑鎓氯化物(2)和硫胺素(3)对人红细胞碳酸酐酶 I、II 同工酶(hCA I 和 hCA II)和分泌同工酶 CA VI 的体外抑制作用。对于 hCA I,K(i) 值范围为 0.38 至 2.27 µM,对于 hCA II,K(i) 值范围为 0.085 至 0.784 µM,对于 hCA VI,K(i) 值范围为 0.062 至 0.593 µM。这些化合物对 hCA II 表现出相对较强的作用,与临床使用的磺胺类药物乙氧唑胺、佐尼沙胺和乙酰唑胺处于同一范围。