Synthesis and biological evaluation of 1-(4-(piperazin-1-yl)phenyl) pyridin-2(1H)-one derivatives as potential SSRIs

被引：10
|
作者：
Xu, Tengfei [1 ,2 ]
Xue, Yaping [1 ,2 ]
Lu, Jielian [1 ,2 ]
Jin, Chuanfei [1 ,2 ]
机构：
[1] Sunshine Lake Pharma Co Ltd, Shenzhen 518000, Peoples R China
[2] HEC Pharm Grp, HEC Res & Dev Ctr, Dongguan 523871, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2021年 / 223卷
关键词：
Serotonin reuptake inhibition; 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives; Antidepressant; MAJOR DEPRESSIVE DISORDER; SEROTONIN; NOREPINEPHRINE; DISCOVERY; ANTIDEPRESSANTS; VILAZODONE; REUPTAKE; EFFICACY; NETWORK; ADULTS;
D O I：
10.1016/j.ejmech.2021.113644
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives were synthesized and evaluated for their serotonin (5-HT) reuptake inhibitory activity. The results in vitro indicated that most of the evaluated compounds displayed potent 5-HT reuptake inhibition. The most promising compound A20 was stable in human liver microsomes and possessed good pharmacokinetic properties. Antidepressant study in vivo of the compound A20 showed that A20 could potently antagonize the p-chloroamphetamine (PCA)-induced depletion of serotonin in hypothalamus and reduce immobility times in the rat forced swimming test (FST). (C) 2021 Elsevier Masson SAS. All rights reserved.
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页数：8
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