In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation: Carbon analogs of (−)-cytisine

Bioorganic & Medicinal Chemistry Letters
2005.0

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.

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