Design and synthesis of a novel series of (1′S,2R,4′S)-3H-4′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2′-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor

[Display omitted] We describe an efficient and convergent synthesis of a series of (1′S,2R,4′S)-3H-4′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2′-bicyclo[2.2.2]octanes] displaying potency for the α7 nicotinic acetylcholine receptor (nAChR) and good selectivity vs. the related 5-HT3A receptor....

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-11, Vol.27 (22), p.5002-5005
Hauptverfasser:	Cook, James, Zusi, F. Christopher, Hill, Matthew D., Fang, Haiquan, Pearce, Bradley, Park, Hyunsoo, Gallagher, Lizbeth, McDonald, Ivar M., Bristow, Linda, Macor, John E., Olson, Richard E.
Format:	Artikel
Sprache:	eng
Schlagworte:	5-HT3A receptor alpha7 Nicotinic Acetylcholine Receptor - chemistry alpha7 Nicotinic Acetylcholine Receptor - metabolism Bridged Bicyclo Compounds - chemical synthesis Bridged Bicyclo Compounds - chemistry Bridged Bicyclo Compounds - metabolism Crystallography, X-Ray Drug Design Humans Hydrogen Bonding Molecular Conformation Nicotinic Agonists - chemistry Nicotinic Agonists - metabolism Octanes - chemical synthesis Octanes - chemistry Octanes - metabolism Protein Binding Receptors, Serotonin, 5-HT3 - chemistry Receptors, Serotonin, 5-HT3 - metabolism Schizophrenia Spirooxazolines Stereoisomerism α7 nicotinic acetylcholine receptor
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Zusammenfassung:	[Display omitted] We describe an efficient and convergent synthesis of a series of (1′S,2R,4′S)-3H-4′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2′-bicyclo[2.2.2]octanes] displaying potency for the α7 nicotinic acetylcholine receptor (nAChR) and good selectivity vs. the related 5-HT3A receptor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.10.009