title: Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives.
abstract: The synthesis and SAR of novel highly potent and selective dopamine D(3)-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED(50) 6.1mg/kg po), a social interaction paradigm.
authors.affiliation: Abbott GmbH & Co. KG, Discovery Research, D-67008 Ludwigshafen, Germany. herve.geneste@abbott.com
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: Andreas
authors.initials: A
authors.lastname: Kling
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; D001578:Benzopyrans / Q000037:antagonists & inhibitors; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D008956:Models, Chemical; D010078:Oxazines / Q000037:antagonists & inhibitors; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: C508939:A-690344; D001578:Benzopyrans; D018492:Dopamine Antagonists; D010078:Oxazines; D011744:Pyrimidinones; D050637:Receptors, Dopamine D3; C062458:3,4,4a,10b-tetrahydro-4-propyl-2H,5H-(1)benzopyrano(4,3-b)-1,4-oxazin-9-ol