Acetylcholinesterase inhibition by fused dihydroquinazoline compounds

被引：60

作者：

Jaen, JC ^{[1
]}

Gregor, VE ^{[1
]}

Lee, C ^{[1
]}

Davis, R ^{[1
]}

Emmerling, M ^{[1
]}

机构：

[1] WARNER LAMBERT PARKE DAVIS, DIV PHARMACEUT RES DIV, DEPT PHARMACOL, ANN ARBOR, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 06期

关键词：

D O I：

10.1016/0960-894X(96)00102-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new type of dihydroquinazoline-based inhibitor of acetylcholinesterase (AChE) is described. These compounds were designed to interact with the catalytic site of AChE in a manner similar to the known inhibitor tacrine, In a manner analogous to the potency enhancement obtained by addition of chlorine atoms to the tacrine molecule, a 3-chloro derivative of the parent hexahydroazepino[2,1-b]quinazoline structure was found to be about 8 times more potent as an AChE inhibitor than the unsubstituted compound.

引用

页码：737 / 742

页数：6

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