Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374180 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
Several N-pyridin-3-yl spirobicyclic diamines, designed as conformationally restricted analogs of tebanicline (ABT-594), were synthesized as novel ligands for nicotinic acetylcholine receptors (nAChR). The spirocyclic compounds exhibited weaker binding affinity, than other constrained analogs in accord with a pharmacophore model. Nevertheless, some (1a, 1b) possessed (partial) agonist potencies comparable to nicotine at the α4β2 subtype, but with greatly improved selectivity relative to the α3β4* nAChR.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kevin B. Sippy, David J. Anderson, William H. Bunnelle, Charles W. Hutchins, Michael R. Schrimpf,