Potent dihydroquinolinone dopamine D sub(2) partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia

A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D sub(2) ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D sub(2) partial agon...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 9; pp. 2983 - 2986
Main Authors Yan, Yinfa, Zhou, Ping, Rotella, David P, Feenstra, Rolf, Kruse, Chris G, Reinders, Jan-Hendrik, Van der Neut, Martina, Lai, Margaret, Zhang, Jean, Kowal, Dianne M, Carrick, Tikva, Marquis, Karen L, Pausch, Mark H, Robichaud, Albert J
Format Journal Article
LanguageEnglish
Published 01.05.2010
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Summary:A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D sub(2) ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D sub(2) partial agonists and serotonin reuptake inhibitors. Structure-activity studies revealed that the linker plays a key role in contributing to D sub(2) affinity, function, and SRI activity.
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SourceType-Scholarly Journals-1
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.02.105