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Structure-Activity Studies of 7-Heteroaryl-3-azabicyclo[3.3.1]non-6-enes: A Novel Class of Highly Potent Nicotinic Receptor Ligands.
MedLine Citation:
PMID:  23025891     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
The potential for nicotinic ligands with affinity for the α4β2 or α7 subtypes to treat such diverse diseases as nicotine addiction, neuropathic pain, neurodegenerative and cognitive disorders has been exhibited clinically for several compounds while preclinical activity in relevant in vivo models has been demonstrated for many more. For several therapeutic programs, we sought nicotinic ligands with various combinations of affinity and function across both subtypes, with an emphasis on dual α4β2 - α7 ligands, to explore the possibility of synergistic effects. We report here the Structure-Activity Relationships (SAR) for a novel series of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes and characterize many of the analogs for activity at additional nicotinic subtypes.
Authors:
Scott R Breining; Matthew S Melvin; Balwinder S Bhatti; Gary D Byrd; Melanie N Kiser; Christopher D Hepler; Dawn N Hooker; Jenny Zhang; Leslie A Reynolds; Lisa R Benson; Nikolai B Fedorov; Serguei S Sidach; J Pike Mitchener; Linda M Lucero; Ronald J Lukas; Paul Whiteaker; Daniel Yohannes
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-10-1
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Oct 
Date Detail:
Created Date:  2012-10-2     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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