4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: Design, synthesis and structure-activity relationships

被引：16
|
作者：
Fish, Paul V. [1 ]
Andrews, Mark D. [1 ]
Fray, M. Jonathan [1 ]
Stobie, Alan [1 ]
Wakenhut, Florian [1 ]
Whitlock, Gavin A. [1 ]
机构：
[1] Pfizer Global Res & Dev, Sandwich Labs, Discovery Chem, Sandwich CT13 9NJ, Kent, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 10期
关键词：
Dual SNRI; Selective SRI; Selective NRI; Triple SNDRI; 4-Piperidine; 3-Piperidine; 3-Pyrrolidine; Monoamine reuptake inhibitor; DERIVATIVES; NOREPINEPHRINE; DRUGS;
D O I：
10.1016/j.bmcl.2009.03.090
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Single enantiomer [(aryloxy)(pyridinyl) methyl] piperidine and pyrrolidine derivatives 5-9 are inhibitors of monoamine reuptake. Structure-activity relationships established that monoamine reuptake inhibition are functions of amine, pyridine isomer, aryloxy ring substitution and stereochemistry. Consequently, selective NRIs, selective SRIs, dual SNRIs and triple SNDRIs were all identified. Dual SNRIs 51-a and 9c were evaluated in additional pharmacology and pharmacokinetic studies as representative examples from this series. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2829 / 2834
页数：6
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