期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 23, 页码 6604-6607出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.014
关键词
Norepinephrine reuptake inhibitor; NRI; 5-HT1A agonist; NET; DAT; SERT; 5-Hydroxytryptamine 1A; ADHD; Depression
Compounds that are both norepinephrine reuptake inhibitors (NRI) and 5-HT1A partial agonists may have the potential to treat neuropsychiatric disorders including attention deficit hyperactivity disorder (ADHD) and depression. Targeted screening of NRI-active compounds for binding to the 5-HT1A receptor provided a series of thiomorpholinone hits with this dual activity profile. Several iterations of design, synthesis, and testing led to substituted piperidine diphenyl ethers which are potent NRIs with 5-HT1A partial agonist properties. In addition, optimization of these molecules provided compounds which exhibit selectivity for NRI over the dopamine (DAT) and serotonin (SERT) reuptake transporters. Monoamine and 5-HT1A in vitro functional activities for select compounds from the developed piperidine diphenyl ether series are also presented. (C) 2009 Elsevier Ltd. All rights reserved.
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