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

✍ Scribed by Daniel P. Walker; Brad A. Acker; E. Jon Jacobsen; Donn G. Wishka

• Book ID: 102892952
• Publisher: Journal of Heterocyclic Chemistry
• Year: 2008
• Tongue: English
• Weight: 837 KB
• Volume: 45
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.5570450131

✦ Synopsis

Abstract

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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 α7 nicotinic acetylcholine receptor assay as part of a drug discovery program to treat the cognitive deficits in schizophrenia. All new amides showed significant α7 nAChR activity and one series displayed potent α7 activity equal to the quinuclidine series.