| Literature DB >> 16413778 |
Manuel J Cases-Thomas1, John J Masters, Magnus W Walter, Gordon Campbell, Louise Haughton, Peter T Gallagher, David R Dobson, Vincent Mancuso, Benjamin Bonnier, Thierry Giard, Thierry Defrance, Michel Vanmarsenille, Andrew Ledgard, Craig White, Sivi Ouwerkerk-Mahadevan, Francoise J Brunelle, Nancy A Dezutter, Camy A Herbots, Joel Y Lienard, Jeremy Findlay, Lorna Hayhurst, John Boot, Linda K Thompson, Susan Hemrick-Luecke.
Abstract
A novel series of tertiary alcohol containing 2-substituted benzyl morpholines have been discovered as potent and selective inhibitors of the norepinephrine transporter. Efficient synthetic routes were developed featuring a highly diastereoselective nucleophilic addition of benzyl Grignard reagents to enantiopure (4-benzylmorpholin-2-yl)phenylmethanone (11) as the key synthetic step. In vitro binding affinity for the norepinephrine, dopamine and serotonin transporters and in vivo examination of a select compound (16) in a pharmacodynamic animal model for norepinephrine reuptake inhibition are presented.Entities:
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Year: 2006 PMID： 16413778 DOI： 10.1016/j.bmcl.2005.12.061
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823