Preparation of Novel Azabicyclic Amines and α7 Nicotinic Acetylcholine Receptor Activity of Derived Aryl Amides.
2008
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.
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