Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/norepinephrine reuptake inhibitors
Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/norepinephrine reuptake inhibitors
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DOI：
10.1016/j.bmcl.2004.11.025
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发表时间：
2005-02-01
影响因子：
2.7
通讯作者：
Wood, V
中科院分区：
文献类型：
--
作者：
Boot, J;Cases, M;Wood, V
新型芳硫甲基吗啡是一种高效的选择性去甲肾上腺素再摄取抑制剂(NERIS)和双重5-羟色胺/去甲肾上腺素再摄取抑制剂(SRI/NERIS)。目标化合物是通过以羟醛缩合为关键步骤的立体化学多功能合成来制备的。2-甲氧基取代类似物的一个对映体是有效的和选择性的去甲肾上腺素再摄取抑制剂，而相反的对映体是有效的双重5-羟色胺/去甲肾上腺素再摄取抑制剂。(C)2004爱思唯尔有限公司。保留所有权利。
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.