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Preparation of novel azabicyclic amines and α7 nicotinic acetylcholine receptor activity of derived aryl amides
Author(s) -
Walker Daniel P.,
Acker Brad A.,
Jon Jacobsen E.,
Wishka Donn G.
Publication year - 2008
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570450131
Subject(s) - chemistry , quinuclidine , nonane , octane , nicotinic agonist , aryl , stereochemistry , dabco , nicotinic acetylcholine receptor , receptor , organic chemistry , biochemistry , alkyl
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.