ChemInform Abstract: 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
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ChemInform Abstract
The title derivatives (δ-lactams) (VIII) and (X) are designed, synthesized, and identified as D2/D4 receptor antagonists. Furthermore, to study the role of the lactam system, the γ-lactam (XII) and the ε-lactam (XV) are prepared by direct condensation of the substituted phenylpiperazines with the corresponding α-halogen lactams. The six-membered ring lactams exhibit appreciable affinities for dopamine receptors; δ-lactams (X) possess more potent D2 and D4 affinity binding and better α1 profile than clozapine.
