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

页码：699 / 703

页数：5

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