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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

Authors :
Hyunsoo Park
James H. Cook
Ivar M. McDonald
Bradley C. Pearce
Matthew D. Hill
Haiquan Fang
John E. Macor
Lizbeth Gallagher
F. Christopher Zusi
Richard E. Olson
Linda J. Bristow
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.

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