Carbonic anhydrase inhibitors: Synthesis and inhibitory properties of 1,3,4-thiadiazole-2,5-bissulfonamide

被引：66

作者：

Supuran, CT ^{[1
]}

Conroy, CW ^{[1
]}

Maren, TH ^{[1
]}

机构：

[1] UNIV FLORIDA, COLL MED, DEPT PHARMACOL & THERAPEUT, GAINESVILLE, FL 32610 USA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 31卷 / 11期

关键词：

carbonic anhydrase; disulfonamide; inhibitor;

D O I：

10.1016/S0223-5234(97)89847-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1,3,4-Thiadiazole-2,5-bissulfonamide was prepared from 2,5-dimercapto-1,3,4-thiadiazole, by a modification of the reported literature procedure, ie, via the sulfenamide. This compound is the lead molecule for designing important classes of pharmacological agents, such as benzothiadiazine diuretics, and it seems to behave as a strong inhibitor of the zinc enzyme carbonic anhydrase (CA). Here we prove that the title compound is actually a weak CA inhibitor and try to explain why previous investigators obtained erroneous data.

引用

页码：843 / 846

页数：4