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.

Authors :: Cook J
Zusi FC
Hill MD
Fang H
Pearce B
Park H
Gallagher L
McDonald IM
Bristow L
Macor JE
Olson RE
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Nov 15; Vol. 27 (22), pp. 5002-5005. Date of Electronic Publication: 2017 Oct 10.
Publication Year :: 2017
Abstract: 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-HT <subscript>3A</subscript> receptor.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)

Subjects :: Bridged Bicyclo Compounds chemical synthesis
Bridged Bicyclo Compounds chemistry
Crystallography, X-Ray
Humans
Hydrogen Bonding
Molecular Conformation
Nicotinic Agonists chemistry
Nicotinic Agonists metabolism
Octanes chemical synthesis
Octanes chemistry
Protein Binding
Receptors, Serotonin, 5-HT3 chemistry
Receptors, Serotonin, 5-HT3 metabolism
Stereoisomerism
alpha7 Nicotinic Acetylcholine Receptor chemistry
Bridged Bicyclo Compounds metabolism
Drug Design
Octanes metabolism
alpha7 Nicotinic Acetylcholine Receptor metabolism

Full Text Access

Tools