Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors

…, DJ Anderson, WH Bunnelle, CW Hutchins…

Index: Sippy, Kevin B.; Anderson, David J.; Bunnelle, William H.; Hutchins, Charles W.; Schrimpf, Michael R. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 6 p. 1682 - 1685

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Citation Number: 15

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 ...