SAR of novel biarylmethylamine dopamine D4 receptor ligands.
SAR for a novel series of dopamine D4 receptor ligands is shown. Very selective, highly potent compounds like 1-(2-pyrimidinyl)-4-(3-(3-thienyl)-benzyl)-piperazine (5f) and 2-(4-(1-fluorenylmethyl)-1-piperazinyl)-pyrimidine (8c) were obtained.
Arlt
M
M
Med Chem ZNS, Darmstadt, Germany. m_arlt@merck.de
Böttcher
H
H
Riethmüller
A
A
Schneider
G
G
Bartoszyk
G D
GD
Greiner
H
H
Seyfried
C A
CA
D000818:Animals; D018492:Dopamine Antagonists / Q000378:metabolism / Q000494:pharmacology; D008024:Ligands; D008744:Methylamines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D051379:Mice; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship
D018492:Dopamine Antagonists; C493600:Drd4 protein, mouse; D008024:Ligands; D008744:Methylamines; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4; C027451:methylamine