Preparation of novel azabicyclic arnines and α7 nicotinic acetylcholine receptor activity of derived aryl amides

被引：6

作者：

Walker, Daniel P. ^{[1
]}

Acker, Brad A. ^{[1
]}

Jacobsen, E. Jon ^{[1
]}

Wishka, Donn G. ^{[1
]}

机构：

[1] Pfizer Inc, Pfizer Global Res & Dev, Chesterfield, MO 63017 USA

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2008年 / 45卷 / 01期

关键词：

D O I：

10.1002/jhet.5570450131

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Three new azabicyclic amines, namely exo-3-amino-1-azabicyclo[3.2.1]octane, 3-amino-1-azabicyclo[3.2.2]nonane and exo-6-amino-8-azabicyclo[3.2.1]octane, have been designed and prepared as isosteres of 3-aminoquinuclidine. Aryl amides derived from each series were prepared and tested in an alpha 7 nicotinic acetylcholine receptor assay as part of a drug discovery program to treat the cognitive deficits in schizophrenia. All new amides showed significant alpha 7 nAChR activity and one series displayed potent alpha 7 activity equal to the quinuclidine series.

引用

页码：247 / 257

页数：11

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