Synthesis and investigation of inhibition effects of new carbonic anhydrase inhibitors

被引：20

作者：

Arslan, O ^{[1
]}

Kufrevioglu, OI ^{[1
]}

Nalbantoglu, B ^{[1
]}

机构：

[1] ATATURK UNIV,FAC SCI & ARTS,DEPT CHEM,ERZURUM,TURKEY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 03期

关键词：

carbonic anhydrase isozymes; carbonic anhydrase inhibitors; OCULAR PHARMACOLOGY; PRESSURE; BINDING; EYE; CO2;

D O I：

10.1016/S0968-0896(96)00272-6

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：

Three new derivatives of 2-substituted 1,3,4-thiadiazole-5-sulfonamide have been synthesized. These compounds are 2-(3-chloropropionylamino)-1,3,4-thiadiazole-5-sulfonamide (1); 2-(2,2-dichloroacetylamino)-1,3,4-thiadiazole-5-sulfonamide (2); and 2-(3-phenylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide (3). Inhibition effects of these compounds on carbonic anhydrase I and II have been investigated. By comparing I-50 and K-i values of the compounds, it has been found that compound 1 is a more potent inhibitor than acetazolamide (b) on carbonic anhydrase II. (C) 1997 Elsevier Science Ltd.

引用

页码：515 / 518

页数：4

共 24 条

[1]

Arslan O., 1996, Turkish Journal of Medical Sciences, V26, P163

[2] THE MECHANISM OF THE FALL IN INTRAOCULAR PRESSURE INDUCED BY THE CARBONIC ANHYDRASE INHIBITOR, DIAMOX [J].