A solid phase parallel synthesis of diverse amides as dopamine D3 receptor ligands.
A solid phase parallel synthesis using SynPhase technology was used to couple a series of 21 carboxylic with three different 4-(4-arylpiperazinyl)butanamines. The resulting library was evaluated as dopamine D(3) receptor ligands giving rise to several compounds with affinities in the low nanomolar concentration range (9e and 9n with binding affinities at D(3) receptors of 0.10 and 0.35 nM respectively).
Jean
Mickaël
M
UPRES EA 4090, Substances licheniques et photoprotection, Faculte des Sciences Biologiques et Medicales, Universite de Rennes I, Rennes, France.
Renault
Jacques
J
Camelin
Jean-Claude
JC
Levoin
Nicolas
N
Danvy
Denis
D
Stark
Holger
H
Capet
Marc
M
Uriac
Philippe
P
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry; D000588:Amines / Q000737:chemistry; D000818:Animals; D002264:Carboxylic Acids / Q000737:chemistry; D006801:Humans; D008024:Ligands; D050637:Receptors, Dopamine D3 / Q000737:chemistry*; D054852:Small Molecule Libraries / Q000138:chemical synthesis*
D000577:Amides; D000588:Amines; D002264:Carboxylic Acids; D008024:Ligands; D050637:Receptors, Dopamine D3; D054852:Small Molecule Libraries