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

doi:10.1002/JHET.5570450131

Paper

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

Published 2008 · Daniel P. Walker, Brad A. Acker, E. Jacobsen

Journal of Heterocyclic Chemistry

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7

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Abstract

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.

In Vitro Study

Study Snapshot

Novel azabicyclic amines show significant 7 nicotinic acetylcholine receptor activity, potentially aiding in schizophrenia drug discovery.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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

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