Structure-activity relationships of KATP channel openers

被引：24

作者：

Mannhold, R ^{[1
]}

机构：

[1] Univ Dusseldorf, Dept Laser Med, Mol Drug Res Grp, D-40225 Dusseldorf, Germany

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2006年 / 6卷 / 10期

关键词：

K-ATP channel openers (KCOs); structure-activity relationships; benzopyrans; cyanoguanidines; thioformamides; diazoxide; cyclobutenediones; dihydropyridine related structures; tertiary carbinols;

D O I：

10.2174/156802606777323647

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Given their many physiological functions, K-ATP channels represent promising drug targets. Sulfonylureas like glibenclamide block KATP channels; they are used in the therapy of type 2 diabetes. Openers of K-ATP channels (KCOs) e.g. relax smooth Muscle and induce hypotension. KCOs are chemically heterogeneous and include as different classes as the benzopyrans, cyanoguanidines, thioformamides, thiadiazines and pyridyl nitrates. Examples for new chemical entities more recently developed as KCOs include cyclobutenediones, dihydropyridine related structures, and tertiary carbinols. Structure-activity relationships of the main chemical classes of KCOs are discussed.

引用

页码：1031 / 1047

页数：17

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