期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 9, 页码 3116-3120出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm9003126
关键词
-
资金
- 6th Framework Programme of the European Union (DeZnIT project)
The Rv3273 gene product of Mycobacterium tuberculosis, beta-carbonic anhydrase (CA, EC 4.2.1.1), mtCA 3, shows appreciable catalytic activity for CO2 hydration (k(cat) of 4.3 x 10(5) s(-1), and k(cat)/K-m of 4.0 x 10(7) M-1.s(-1)). A series of sulfonamides/sulfamates was assayed for their interaction with mtCA 3. Sulfanilyl-sulfonamides, acetazolamide, methazolamide, ethoxzolamide; dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and zonisamide, showed effective, submicromolar inhibition (K(I)s of 104-611 nM), the best inhibitor being 2-amino-pyrimidin-4-yl-sulfanilamide (K-I of 91 nM).
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