Acetylcholinesterase inhibitors based on carbamic acid quinolin-6-yl esters - Council of Scientific and Industrial Research: US20060142335

被引：1

作者：

Decker, Michael ^{[1
]}

机构：

[1] Harvard Univ, Sch Med, Med Chem Lab, Alcohol & Drug Abuse Res Ctr,McLean Hosp, Belmont, MA 02478 USA

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2007年 / 17卷 / 06期

关键词：

acetylcholinesterase (AChE) inhibitor; carbamic acid esters; dementia; peripheral effects of AChE; quinolin-6-ols; 1,2,3,4-tetrahydroquinolin-6-ols;

D O I：

10.1517/13543776.17.6.733

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The application claims two related kinds of carbamic acid esters, namely the ones of quinolin-6-ol and 1-substituted 1,2,3,4-tetrahydroquinolin-6-ols as novel inhibitors of acetylcholinesterase. Hexyl-, heptyl- and substituted phenylcarbamic acids were prepared, in which the 1-position of the tetrahydroquinolinol was either unsubstituted or bore a methyl or benzyl group. Some data concerning their in vitro inhibition are presented, as is the testing of a set of compounds in an in vivo assay (amelioration of scopolamine-induced cognitive impairment in a passive avoidance test), in which the compounds tested showed cognitive improvements comparable to standard Alzheimer's disease drugs. These compounds are among the few patents with novel templates for acetylcholinesterase-inhibiting carbamates described in the past 3 years.

引用

页码：733 / 736

页数：4

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