| Title : Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent alpha4beta2 nicotinic acetylcholine receptor ligands - Scanio_2011_J.Med.Chem_54_7678 |
| Author(s) : Scanio MJ , Shi L , Bunnelle WH , Anderson DJ , Helfrich RJ , Malysz J , Thorin-Hagene KK , Van Handel CE , Marsh KC , Lee CH , Gopalakrishnan M |
| Ref : Journal of Medicinal Chemistry , 54 :7678 , 2011 |
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Abstract :
A series of diazabicyclo[3.3.0]octane substituted pyridines and pyrazines was synthesized and characterized at the alpha4beta2 neuronal nicotinic acetylcholine receptor (nAChR). The compounds were designed to mimic the profile of ABT-089, high affinity binding ligand for the alpha4beta2 nAChR, with limited agonist activity. Carboxamide derivatives of 3-(diazabicyclo[3.3.0]octane)-substituted pyridines or 2-(diazabicyclo[3.3.0]octane)-substituted pyrazines were found to have the desired binding and activity profile. The structure-activity relationship of these compounds is presented. |
| PubMedSearch : Scanio_2011_J.Med.Chem_54_7678 |
| PubMedID: 21962147 |
Scanio MJ, Shi L, Bunnelle WH, Anderson DJ, Helfrich RJ, Malysz J, Thorin-Hagene KK, Van Handel CE, Marsh KC, Lee CH, Gopalakrishnan M (2011)
Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent alpha4beta2 nicotinic acetylcholine receptor ligands
Journal of Medicinal Chemistry
54 :7678
Scanio MJ, Shi L, Bunnelle WH, Anderson DJ, Helfrich RJ, Malysz J, Thorin-Hagene KK, Van Handel CE, Marsh KC, Lee CH, Gopalakrishnan M (2011)
Journal of Medicinal Chemistry
54 :7678