Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/norepinephrine reuptake inhibitors

被引：30
|
作者：
Boot, J
Cases, M
Clark, BP
Findlay, J
Gallagher, PT
Hayhurst, L
Man, T
Montalbetti, C
Rathmell, RE
Rudyk, H
Walter, MW
Whatton, M
Wood, V
机构：
[1] Eli Lilly & Co, Lilly Res Ctr, Windlesham GU20 6PH, Surrey, England
[2] Evotec OAI, Abingdon OX14 4SD, Oxon, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 03期
关键词：
monoamine reuptake inhibitors; selective norepinephrine reuptake inhibitor; dual reuptake inhibitor; SAR; serotonin; norepinephrine;
D O I：
10.1016/j.bmcl.2004.11.025
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel arylthiomethyl morpholines are potent selective norepinephrine reuptake inhibitors (NERIs) and dual serotonin/ norepinephrine reuptake inhibitors (SRI/NERIs). The target compounds were prepared using a stereochemically versatile synthesis featuring an aldol condensation as the key step. One enantiomer of the 2-methoxy-substituted analogue was found to be a potent and selective norepinephrine reuptake inhibitor, whereas the opposite enantiomer was a potent dual serotonin/norepinephrine reuptake inhibitor. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：699 / 703
页数：5
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