Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379699 | Bioorganic & Medicinal Chemistry Letters | 2005 | 6 Pages |
Abstract
The preparation and biological activity of analogs of (−)-cytisine, an α4β2 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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Organic Chemistry
Authors
Jotham W. Coe, Michael G. Vetelino, Crystal G. Bashore, Michael C. Wirtz, Paige R. Brooks, Eric P. Arnold, Lorraine A. Lebel, Carol B. Fox, Steven B. Sands, Thomas I. Davis, David W. Schulz, Hans Rollema, F. David Tingley III, Brian T. O’Neill,