Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel α7 neuronal nicotinic receptor (NNR) ligands

被引：9

作者：

Li, Tao ^{[1
]}

Bunnelle, William H. ^{[1
]}

Ryther, Keith B. ^{[1
]}

Anderson, David J. ^{[1
]}

Malysz, John ^{[1
]}

Helfrich, Rosalind ^{[1
]}

Gronlien, Jens H. ^{[1
]}

Hakerud, Monika ^{[1
]}

Peters, Dan ^{[2
]}

Schrimpf, Michael R. ^{[1
]}

Gopalakrishnan, Murali ^{[1
]}

Ji, Jianguo ^{[1
]}

机构：

[1] Abbott, GPRD, Neurosci Res, Abbott Pk, IL 60064 USA

[2] NeuroSearch AS, DK-2750 Ballerup, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 12期

关键词：

2,5-Diazabicyclo[2.2.1]heptanes; Neuronal nicotinic receptors; NNRs; alpha; 7; Cognitive deficits; ACETYLCHOLINE-RECEPTORS; DERIVATIVES; AGONISTS; BINDING;

D O I：

10.1016/j.bmcl.2010.04.105

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha 7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha 7 NNR agonist activity. (C) 2010 Elsevier Ltd. All rights reserved.

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收藏

页码：3636 / 3639

页数：4

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