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 evaluation.
Jean
Mickaël
M
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.
Renault
Jacques
J
Levoin
Nicolas
N
Danvy
Denis
D
Calmels
Thierry
T
Berrebi-Bertrand
Isabelle
I
Robert
Philippe
P
Schwartz
J C
JC
Lecomte
J M
JM
Uriac
Philippe
P
Capet
Marc
M
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D051379:Mice; D008958:Models, Molecular; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D051381:Rats; D050637:Receptors, Dopamine D3 / Q000378:metabolism*
D000577:Amides; D008024:Ligands; D010879:Piperazines; D050637:Receptors, Dopamine D3; D000077489:Piperazine