Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594029 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
A series of racemic N-arylalkyl-2-azaadamantan-1-ols (9-15) and the corresponding deoxygenated, achiral N-arylalkyl-2-azaadamantanes (23-29) were synthesized and screened in competition binding assays against a panel of CNS targets. Adamantyl hemiaminals 9-15 displayed generally low affinity for both Ï1 (Ki values = 294-1950 nM) and Ï2 receptors (Ki values = 201-1020 nM), and negligible affinity for 42 other CNS proteins. Deoxygenation of 9-15 to give the corresponding achiral azaadamantanes 23-29 greatly improved affinity for Ï1 (Ki values = 8.3-239 nM) and Ï2 receptors (Ki values = 34-312 nM).
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Samuel D. Banister, David T. Yoo, Sook Wern Chua, Jinquan Cui, Robert H. Mach, Michael Kassiou,