Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands

Mickaël Jean; Jacques Renault; Nicolas Levoin; Denis Danvy; Thierry Calmels; Isabelle Berrebi-Bertrand; Philippe Robert; J C Schwartz; J M Lecomte; Philippe Uriac; Marc Capet

doi:10.1016/j.bmcl.2010.07.096

Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5376-9. doi: 10.1016/j.bmcl.2010.07.096. Epub 2010 Jul 29.

Authors

Mickaël Jean¹, Jacques Renault, Nicolas Levoin, Denis Danvy, Thierry Calmels, Isabelle Berrebi-Bertrand, Philippe Robert, J C Schwartz, J M Lecomte, Philippe Uriac, Marc Capet

Affiliation

¹ UPRES EA 4090, Substances Lichéniques et Photoprotection, Université de Rennes I, Faculté des Sciences Biologiques et Médicales, 2, Av. du Pr. Léon Bernard, 35043 Rennes, France.

PMID: 20708933
DOI: 10.1016/j.bmcl.2010.07.096

Abstract

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.

MeSH terms

Amides / chemical synthesis
Amides / chemistry*
Amides / pharmacokinetics*
Amides / pharmacology
Animals
Brain / metabolism*
Humans
Ligands
Mice
Models, Molecular
Piperazine
Piperazines / chemical synthesis
Piperazines / chemistry*
Piperazines / pharmacokinetics*
Piperazines / pharmacology
Rats
Receptors, Dopamine D3 / metabolism*

Substances

Amides
Ligands
Piperazines
Receptors, Dopamine D3
Piperazine