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Design and synthesis of a novel series of (1′ S ,2 R ,4′ S )-3 H -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
- Source :
- Bioorganic & Medicinal Chemistry Letters. 27:5002-5005
- Publication Year :
- 2017
- Publisher :
- Elsevier BV, 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-HT3A receptor.
- Subjects :
- 0301 basic medicine
alpha7 Nicotinic Acetylcholine Receptor
Stereochemistry
Clinical Biochemistry
Molecular Conformation
Convergent synthesis
Pharmaceutical Science
Crystallography, X-Ray
01 natural sciences
Biochemistry
Bridged Bicyclo Compounds
03 medical and health sciences
chemistry.chemical_compound
α7 nicotinic acetylcholine receptor
Drug Discovery
Humans
Potency
Nicotinic Agonists
Receptor
Molecular Biology
Oxazole
Bicyclic molecule
Organic Chemistry
Hydrogen Bonding
Stereoisomerism
Octanes
0104 chemical sciences
010404 medicinal & biomolecular chemistry
030104 developmental biology
Nicotinic agonist
chemistry
Drug Design
Molecular Medicine
Receptors, Serotonin, 5-HT3
Selectivity
Protein Binding
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 27
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....67c17ad27adf8439455974f7b5770b18
- Full Text :
- https://doi.org/10.1016/j.bmcl.2017.10.009