In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation:: Carbon analogs of (-)-cytisine

被引：55

作者：

Coe, JW ^{[1
]}

Vetelino, MG ^{[1
]}

Bashore, CG ^{[1
]}

Wirtz, MC ^{[1
]}

Brooks, PR ^{[1
]}

Arnold, EP ^{[1
]}

Lebel, LA ^{[1
]}

Fox, CB ^{[1
]}

Sands, SB ^{[1
]}

Davis, TI ^{[1
]}

Schulz, DW ^{[1
]}

Rollema, H ^{[1
]}

Tingley, FD ^{[1
]}

O'Neill, BT ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton Labs, Eastern Point Rd, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 12期

关键词：

alpha 4 beta 2 nicotinic receptor; nAChR; partial agonist; smoking; cessation; alkaloid;

D O I：

10.1016/j.bmcl.2005.04.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The preparation and biological activity of analogs of (-)-cytisine, an alpha 4 beta 2 nicotinic receptor partial agonist, are discussed. All-carbon-containing phenyl ring replacements of the pyridone ring system, generated via Heck cyclization protocols, exhibited weaker affinity and lower efficacy partial agonist profiles relative to (-)-cytisine. In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (-)-cytisine. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：2974 / 2979

页数：6

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