| Title : In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine - Coe_2005_Bioorg.Med.Chem.Lett_15_2974 |
| Author(s) : 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, 3rd , O'Neill BT |
| Ref : Bioorganic & Medicinal Chemistry Lett , 15 :2974 , 2005 |
|
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. |
| PubMedSearch : Coe_2005_Bioorg.Med.Chem.Lett_15_2974 |
| PubMedID: 15908213 |
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, 3rd, O'Neill BT (2005)
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine
Bioorganic & Medicinal Chemistry Lett
15 :2974
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, 3rd, O'Neill BT (2005)
Bioorganic & Medicinal Chemistry Lett
15 :2974