| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374309 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Yinfa Yan, Ping Zhou, David P. Rotella, Rolf Feenstra, Chris G. Kruse, Jan-Hendrik Reinders, Martina van der Neut, Margaret Lai, Jean Zhang, Dianne M. Kowal, Tikva Carrick, Karen L. Marquis, Mark H. Pausch, Albert J. Robichaud,