Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com.
The synthesis and SAR of novel and selective dopamine D(3)-receptor antagonists based on a 3,4-dihydro-1H-quinolin-2-one, a 1,3,4,5-tetrahydro-benzo[b]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzo[b]azepine-2,5-dione scaffold are discussed. A706149 (2.15mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigm.
Geneste
Hervé
H
Abbott GmbH & Co. KG, Discovery Research, D-67008 Ludwigshafen, Germany.
Backfisch
Gisela
G
Braje
Wilfried
W
Delzer
Jürgen
J
Haupt
Andreas
A
Hutchins
Charles W
CW
King
Linda L
LL
Lubisch
Wilfried
W
Steiner
Gerd
G
Teschendorf
Hans-Jürgen
HJ
Unger
Liliane
L
Wernet
Wolfgang
W
D000818:Animals; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D001552:Benzazepines; D018492:Dopamine Antagonists; D015363:Quinolones; D050637:Receptors, Dopamine D3