Title

Potent Dihydroquinolinone Dopamine D2 Partial Agonist/Serotonin Reuptake Inhibitors for the Treatment of Schizophrenia

Document Type

Article

Publication Date

5-1-2010

Abstract

A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D2 ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D2 partial agonists and serotonin reuptake inhibitors. Structure-activity studies revealed that the linker plays a key role in contributing to D2 affinity, function, and SRI activity.

DOI

10.1016/j.bmcl.2010.02.105

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