title: 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.
abstract: 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.
authors.affiliation: Abbott GmbH & Co. KG, Discovery Research, D-67008 Ludwigshafen, Germany.
authors.forename: Hervé
authors.initials: H
authors.lastname: Geneste
authors.forename: Gisela
authors.initials: G
authors.lastname: Backfisch
authors.forename: Wilfried
authors.initials: W
authors.lastname: Braje
authors.forename: Jürgen
authors.initials: J
authors.lastname: Delzer
authors.forename: Andreas
authors.initials: A
authors.lastname: Haupt
authors.forename: Charles W
authors.initials: CW
authors.lastname: Hutchins
authors.forename: Linda L
authors.initials: LL
authors.lastname: King
authors.forename: Wilfried
authors.initials: W
authors.lastname: Lubisch
authors.forename: Gerd
authors.initials: G
authors.lastname: Steiner
authors.forename: Hans-Jürgen
authors.initials: HJ
authors.lastname: Teschendorf
authors.forename: Liliane
authors.initials: L
authors.lastname: Unger
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Wernet
mesh_terms: 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
chemical_list: D001552:Benzazepines; D018492:Dopamine Antagonists; D015363:Quinolones; D050637:Receptors, Dopamine D3