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

被引：20

作者：

Ozdemir, Zafer Omer ^{[1
]}

Senturk, Murat ^{[2
]}

Ekinci, Deniz ^{[3
]}

机构：

[1] Kirklareli Univ, Art & Sci Fac, Dept Chem, Kirklareli, Turkey

[2] Ibrahim Cecen Univ Agri, Art & Sci Fac, Dept Chem, Agri, Turkey

[3] Ondokuz Mayis Univ, Fac Agr, Dept Agr Biotechnol, Samsun, Turkey

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2013年 / 28卷 / 02期

关键词：

Carbonic anhydrase; thiamine; inhibition; VITRO INHIBITION; PHENOLIC-COMPOUNDS; ISOZYME-II; SULFONAMIDES; AGENTS; MOIETIES; BINDING; SERIES;

D O I：

10.3109/14756366.2011.637200

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu M for hCA I, 0.085 to 0.784 mu M for hCA II and 0.062 to 0.593 mu M 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.

引用

页码：316 / 319

页数：4

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