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.
MeSH terms
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Antipsychotic Agents / chemical synthesis
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Antipsychotic Agents / metabolism
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Clozapine / metabolism
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Dopamine D2 Receptor Antagonists
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Humans
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Lactams / chemical synthesis*
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Lactams / metabolism
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Piperazines / chemical synthesis
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Piperazines / metabolism
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Protein Binding
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Quinolones / chemical synthesis
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Quinolones / metabolism
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Receptors, Dopamine / metabolism*
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Receptors, Dopamine D2 / metabolism
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Receptors, Dopamine D4
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Structure-Activity Relationship
Substances
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Antipsychotic Agents
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DRD4 protein, human
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Dopamine D2 Receptor Antagonists
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Lactams
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Piperazines
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Quinolones
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Receptors, Dopamine
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Receptors, Dopamine D2
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Receptors, Dopamine D4
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Clozapine