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

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

  • Bioorg Med Chem Lett. 2009 Mar 15;19(6):1682-5. doi: 10.1016/j.bmcl.2009.01.099.
Kevin B Sippy 1,  David J Anderson,  William H Bunnelle,  Charles W Hutchins,  Michael R Schrimpf
Affiliations

Affiliation

  • 1 Neuroscience Research, Abbott Laboratories, Department R47W, 100 Abbott Park Rd., Building AP9A, Abbott Park, IL 60064-6117, USA.
PMID: 19232492 DOI: 10.1016/j.bmcl.2009.01.099
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 alpha4beta2 subtype, but with greatly improved selectivity relative to the alpha3beta4* nAChR.

Figures