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.
引用
收藏
页码：3636 / 3639
页数：4
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