Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists

被引：9

作者：

Dounay, Amy B. ^{[1
]}

Barta, Nancy S. ^{[2
]}

Campbell, Brian M. ^{[1
]}

Coleman, Corey ^{[1
]}

Collantes, Elizabeth M. ^{[1
]}

Denny, Lynne ^{[2
]}

Dutta, Satavisha ^{[2
]}

Gray, David L. ^{[1
]}

Hou, Dongfeng ^{[3
]}

Iyer, Rathna ^{[1
]}

Maiti, Samarendra N. ^{[3
]}

Ortwine, Daniel F. ^{[2
]}

Probert, Al ^{[1
]}

Stratman, Nancy C. ^{[1
]}

Subedi, Rajendra ^{[3
]}

Whisman, Tammy ^{[1
]}

Xu, Wenjian ^{[1
]}

Zoski, Kim ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton, CT 06340 USA

[2] Pfizer Global Res & Dev, Ann Arbor, MI 48105 USA

[3] Naeja Pharmaceut Res & Dev, Edmonton, AB, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

Norepinephrine reuptake inhibitor; 5-HT1A partial agonist; INTRINSIC CLEARANCE DATA; SEROTONIN; EFFICACY; REBOXETINE; MICROSOMES;

D O I：

10.1016/j.bmcl.2009.12.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Preclinical studies suggest that compounds with dual norepinephrine reuptake inhibitor (NRI) and 5-HT1A partial agonist properties may provide an important new therapeutic approach to ADHD, depression, and anxiety. Reported herein is the discovery of a novel chemical series with a favorable NRI and 5-HT1A partial agonist pharmacological pro. le as well as excellent selectivity for the norepinephrine transporter over the dopamine transporter. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1114 / 1117

页数：4

共 22 条

[1] Recent developments in the design of anti-depressive therapies: Targeting the serotonin transporter [J].