Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands

Isosteric replacement of the amide function and modulation of the arylpiperazine moiety of known dopamine D3 receptor ligands led to potent and selective compounds. Enhanced bioavailability and preferential brain distribution make compound 6c a good candidate for pharmacological and clinical evaluat...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-09, Vol.20 (18), p.5376-5379
Main Authors: Jean, Mickaël, Renault, Jacques, Levoin, Nicolas, Danvy, Denis, Calmels, Thierry, Berrebi-Bertrand, Isabelle, Robert, Philippe, Schwartz, J.C., Lecomte, J.M., Uriac, Philippe, Capet, Marc
Format: Article
Language:English
Subjects:
Amide isoster
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacokinetics
Amides - pharmacology
Animals
Bioavailability
Biological and medical sciences
Brain - metabolism
Catecholaminergic system
Chemical Sciences
Dopamine D3 receptor ligand
Humans
Ligands
Medical sciences
Mice
Models, Molecular
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Organic chemistry
Pharmacology. Drug treatments
Piperazines - chemical synthesis
Piperazines - chemistry
Piperazines - pharmacokinetics
Piperazines - pharmacology
Rats
Receptors, Dopamine D3 - metabolism
Selectivity
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Isosteric replacement of the amide function and modulation of the arylpiperazine moiety of known dopamine D3 receptor ligands led to potent and selective compounds. Enhanced bioavailability and preferential brain distribution make compound 6c a good candidate for pharmacological and clinical evaluation.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.07.096