Diazaspirocyclic compounds as selective ligands for the α4β2 nicotinic acetylcholine receptor

JP Strachan, JJ Farias, J Zhang, WS Caldwell…

文献索引：Strachan, Jon-Paul; Farias, Jarrett J.; Zhang, Jenny; Caldwell, William S.; Bhatti, Balwinder S. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5089 - 5092

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被引用次数: 3

摘要

Diazaspirocyclic ligands have been synthesized in four steps as selective α4β2 nicotinic acetylcholine receptor antagonists. Structural assignment of 1-(pyridin-3-yl)-2- spiropyrrolidino-3, 2′-1-azabiclo [2.2. 1] heptane 2, was confirmed using a combination of NMR experiments on a key intermediate, spirolactam 9. All three target compounds synthesized in this diazaspirocyclic series exhibited high affinity (Ki< 35nM) at the human ...