Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: A novel series of mixed dopamine D2/D4 receptor antagonists

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-3...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-09, Vol.10 (18), p.2119-2122
Main Authors: HE ZHAO, THURKAUF, Andrew, BRAUN, Julia, BRODBECK, Robin, KIELTYKA, Andrzej
Format: Article
Language:English
Subjects:
Antipsychotic Agents - chemical synthesis
Antipsychotic Agents - metabolism
Biological and medical sciences
Catecholaminergic system
Clozapine - metabolism
Dopamine D2 Receptor Antagonists
Humans
Lactams - chemical synthesis
Lactams - metabolism
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Piperazines - chemical synthesis
Piperazines - metabolism
Protein Binding
Quinolones - chemical synthesis
Quinolones - metabolism
Receptors, Dopamine - metabolism
Receptors, Dopamine D2 - metabolism
Receptors, Dopamine D4
Structure-Activity Relationship
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Summary: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.
ISSN:0960-894X
DOI:10.1016/S0960-894X(00)00421-2