Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia

被引：20

作者：

Yan, Yinfa ^{[1
]}

Zhou, Ping ^{[1
]}

Rotella, David P. ^{[1
]}

Feenstra, Rolf ^{[2
]}

Kruse, Chris G. ^{[2
]}

Reinders, Jan-Hendrik ^{[2
]}

van der Neut, Martina ^{[2
]}

Lai, Margaret ^{[3
]}

Zhang, Jean ^{[3
]}

Kowal, Dianne M. ^{[3
]}

Carrick, Tikva ^{[3
]}

Marquis, Karen L. ^{[3
]}

Pausch, Mark H. ^{[3
]}

Robichaud, Albert J. ^{[1
]}

机构：

[1] Wyeth Res, Chem Sci, Princeton, NJ 08543 USA

[2] Solvay Pharmaceut Res Labs, NL-1381 CP Weesp, Netherlands

[3] Wyeth Res, Discovery Neurosci, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 09期

关键词：

Serotonin reuptake inhibitor; Dopamine D-2 partial agonist; Schizophrenia; DEPRESSION; ARIPIPRAZOLE; COMBINATION; OLANZAPINE; FLUOXETINE;

D O I：

10.1016/j.bmcl.2010.02.105

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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-2 ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D-2 partial agonists and serotonin reuptake inhibitors. Structure-activity studies revealed that the linker plays a key role in contributing to D-2 affinity, function, and SRI activity. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2983 / 2986

页数：4

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