Carbonic Anhydrase Inhibitors. Cloning, Characterization, and Inhibition Studies of a New β-Carbonic Anhydrase from Mycobacterium tuberculosis

被引：99

作者：

Nishimori, Isao ^{[2
]}

Minakuchi, Tomoko ^{[2
]}

Vullo, Daniela ^{[1
]}

Scozzafava, Andrea ^{[1
]}

Innocenti, Alessio ^{[1
]}

Supuran, Claudiu T. ^{[1
]}

机构：

[1] Univ Florence, Lab Chim Bioinorgan, I-50019 Florence, Italy

[2] Kochi Med Sch, Dept Gastroenterol, Nanko Ku, Kochi 7838505, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 09期

关键词：

PH-DEPENDENT ACTIVITY; HELICOBACTER-PYLORI; CRYPTOCOCCUS-NEOFORMANS; SULFAMATE INHIBITORS; GENOME SEQUENCE; DNA CLONING; SULFONAMIDE; TARGET; ENZYME; DRUGS;

D O I：

10.1021/jm9003126

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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).

引用

页码：3116 / 3120

页数：5

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