Structure–Activity Studies of Diazabicyclo [3.3. 0] octane-Substituted Pyrazines and Pyridines as Potent α4β2 Nicotinic Acetylcholine Receptor Ligands

…, RJ Helfrich, J Malysz, KK Thorin-Hagene…

文献索引：Scanio, Marc J. C.; Shi, Lei; Bunnelle, William H.; Anderson, David J.; Helfrich, Rosalind J.; Malysz, John; Thorin-Hagene, Kirsten K.; Van Handel, Ceclia E.; Marsh, Kennan C.; Lee, Chih-Hung; Gopalakrishnan, Murali Journal of Medicinal Chemistry, 2011 , vol. 54, # 21 p. 7678 - 7692

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被引用次数: 5

摘要

A series of diazabicyclo [3.3. 0] octane substituted pyridines and pyrazines was synthesized and characterized at the α4β2 neuronal nicotinic acetylcholine receptor (nAChR). The compounds were designed to mimic the profile of ABT-089, high affinity binding ligand for the α4β2 nAChR, with limited agonist activity. Carboxamide derivatives of 3-(diazabicyclo [3.3. 0] octane)-substituted pyridines or 2-(diazabicyclo [3.3. 0] octane)-substituted ...