In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Basic Information
ID: ALA1139609
Journal: Bioorg Med Chem Lett
Title: In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Authors: Coe JW, Vetelino MG, Bashore CG, Wirtz MC, Brooks PR, Arnold EP, Lebel LA, Fox CB, Sands SB, Davis TI, Schulz DW, Rollema H, Tingley FD, O'Neill BT.
Abstract: The preparation and biological activity of analogs of (-)-cytisine, an alpha4beta2 nicotinic receptor partial agonist, are discussed. All-carbon-containing phenyl ring replacements of the pyridone ring system, generated via Heck cyclization protocols, exhibited weaker affinity and lower efficacy partial agonist profiles relative to (-)-cytisine. In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (-)-cytisine.
CiteXplore: 15908213
DOI: 10.1016/j.bmcl.2005.04.036
Patent ID: ┄