title: Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists.
abstract: 3-Piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives (delta-lactams) were designed, synthesized, and identified as a new series of mixed dopamine D2/D4 receptor antagonists. To further the structure-activity relationship (SAR) study, 3-piperazinylindolin-2-ones (gamma-lactams) and 3-piperazinyl-3H,4H,5H-benzo[f]azepin-2-ones (epsilon-lactams) were also prepared and examined.
authors.affiliation: Neurogen Corporation, Branford, CT 06405, USA. hzhao@nrgn.com
authors.forename: H
authors.initials: H
authors.lastname: Zhao
authors.forename: A
authors.initials: A
authors.lastname: Thurkauf
authors.forename: J
authors.initials: J
authors.lastname: Braun
authors.forename: R
authors.initials: R
authors.lastname: Brodbeck
authors.forename: A
authors.initials: A
authors.lastname: Kieltyka
mesh_terms: D014150:Antipsychotic Agents / Q000138:chemical synthesis / Q000378:metabolism; D003024:Clozapine / Q000378:metabolism; D065127:Dopamine D2 Receptor Antagonists; D006801:Humans; D007769:Lactams / Q000138:chemical synthesis* / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis / Q000378:metabolism; D011485:Protein Binding; D015363:Quinolones / Q000138:chemical synthesis / Q000378:metabolism; D011954:Receptors, Dopamine / Q000378:metabolism*; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship
chemical_list: D014150:Antipsychotic Agents; C493599:DRD4 protein, human; D065127:Dopamine D2 Receptor Antagonists; D007769:Lactams; D010879:Piperazines; D015363:Quinolones; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4; D003024:Clozapine