2-(aryloxymethyl)azacyclic analogues as novel nicotinic acetylcholine receptor (nAChR) ligands

被引：23

作者：

Elliott, RL ^{[1
]}

Kopecka, H ^{[1
]}

Gunn, DE ^{[1
]}

Lin, NH ^{[1
]}

Garvey, DS ^{[1
]}

Ryther, KB ^{[1
]}

Holladay, MW ^{[1
]}

Anderson, DJ ^{[1
]}

Campbell, JE ^{[1
]}

Sullivan, JP ^{[1
]}

Buckley, MJ ^{[1
]}

Gunther, KL ^{[1
]}

ONeill, AB ^{[1
]}

Decker, MW ^{[1
]}

Arneric, SP ^{[1
]}

机构：

[1] ABBOTT LABS,DEPT 47W,ABBOTT PK,IL 60064

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 19期

关键词：

D O I：

10.1016/0960-894X(96)00416-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-(aryloxymethyl) azetidine and pyrrolidine nAChR ligands in which the 3-pyridyl moiety of a previously described series(1) was replaced by a substituted phenyl group was explored. Aromatic substitution afforded analogues with K-i values ranging from 3 Co >10,000 nM. Generally, substitution at the ortho- and para-position was unfavorable, whereas electron-withdrawing groups at the meta-position improved the Ki values. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2283 / 2288

页数：6

共 36 条

[1] Novel 3-pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors [J].