| Literature DB >> 23025891 |
Scott R Breining1, Matt 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.
Abstract
The potential for nicotinic ligands with affinity for the α4β2 or α7 subtypes to treat such diverse diseases as nicotine addiction, neuropathic pain, and 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 analogues for activity at multiple nicotinic subtypes.Entities:
Mesh：
Substances：
Year: 2012 PMID： 23025891 DOI： 10.1021/jm3011299
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446