Synthesis and binding studies on a new series of arylpiperazino benzazol-2-one and benzoxazin-3-one derivatives as selective D4 ligands.
A series of new arylpiperazinomethyl derivatives was designed and studied as potential D4 ligands. The synthesis of these compounds required an original synthetic route. Some of the tested compounds were found to be as potent as clozapine at D4 receptors. Moreover, compounds which displayed a high D2/D4 selectivity ratio (>122) were selected for further pharmacological evaluation.
Carato
P
P
lnstitut de Chimie Pharmaceutique Charles Lespagnol, Lille.
Depreux
P
P
Lesieur
D
D
Millan
M
M
Newman-Tancredi
A
A
Rettori
M C
MC
Caignard
D H
DH
D001393:Azoles / Q000138:chemical synthesis* / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D017072:Neostriatum / Q000187:drug effects / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D017448:Receptors, Dopamine D2 / Q000187:drug effects*; D050638:Receptors, Dopamine D4; D013055:Spectrophotometry, Infrared
D001393:Azoles; D018492:Dopamine Antagonists; D008024:Ligands; D010879:Piperazines; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4