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
收藏
页码：247 / 257
页数：11
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