Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates - subtype selective, high affinity α7 nicotinic acetylcholine receptor agonists

被引：11

作者：

O'Donnell, Christopher J. ^{[1
]}

Peng, Langu ^{[1
]}

O'Neill, Brian T. ^{[1
]}

Arnold, Eric P. ^{[1
]}

Mather, Robert J. ^{[1
]}

Sands, Steven B. ^{[1
]}

Shrikhande, Alka ^{[1
]}

Lebel, Lorraine A. ^{[1
]}

Spracklin, Douglas K. ^{[1
]}

Nedza, Frank M. ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Neurosci Med Chem, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

Alpha; 7; Nicotinic acetylcholine receptor; nAChR; SAR; 1,4-Diazabicyclo[3.2.2]nonane phenyl carbamate; Agonist; RAT-BRAIN; IN-VITRO; BINDING; SCHIZOPHRENIA; SITES; ANALOG;

D O I：

10.1016/j.bmcl.2009.06.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4-diazabicyclo[3.2.2]nonane phenyl carbamate series of alpha 7 nAChR agonists is described. The development of the medicinal chemistry strategy and SAR which led to the identification of 5 and 7aa as subtype selective, high affinity alpha 7 agonists as excellent leads for further evaluation is discussed, along with key physicochemical and pharmacokinetic data highlighting their lead potential. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4747 / 4751

页数：5

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