7-azaindole derivatives as potential partial nicotinic agonists

被引：14

作者：

Stoit, Axel R. ^{[1
]}

den Hartog, Arnold P. ^{[1
]}

Mons, Harry ^{[1
]}

van Schaik, Sjoerd ^{[1
]}

Barkhuijsen, Nynke ^{[1
]}

Stroomer, Cees ^{[1
]}

Coolen, Hein K. A. C. ^{[1
]}

Reinders, Jan Hendrik ^{[1
]}

Adolfs, Tiny J. P. ^{[1
]}

van der Neut, Martina ^{[1
]}

Keizer, Hiskias ^{[1
]}

Kruse, Chris G. ^{[1
]}

机构：

[1] Solvay Pharmaceut, Res Labs, NL-1381 CP Weesp, Netherlands

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

azaindole derivatives; partial agonist; nicotinic acetylcholine receptor; cognition; smoke cessation;

D O I：

10.1016/j.bmcl.2007.10.101

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have investigated a series of 7-azaindoles as potential partial agonists of the alpha 4 beta 2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (K-i = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：188 / 193

页数：6

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