Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Bioorg Med Chem Lett ; 16(7): 2022-5, 2006 Apr 01.
Article in English | MEDLINE | ID: mdl-16413778

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.


Subject(s)
Alcohols/chemistry , Morpholines/pharmacology , Norepinephrine Plasma Membrane Transport Proteins/antagonists & inhibitors , Crystallography, X-Ray , Dopamine Plasma Membrane Transport Proteins/antagonists & inhibitors , Morpholines/chemistry
SELECTION OF CITATIONS
SEARCH DETAIL
...