Syntheses and evaluation of novel isoliquiritigenin derivatives as potential dual inhibitors for amyloid-beta aggregation and 5-lipoxygenase

被引：32

作者：

Chen, Yi-Ping ^{[1
,2
]}

Zhang, Zi-Ying ^{[1
]}

Li, Yan-Ping ^{[1
]}

Li, Ding ^{[1
]}

Huang, Shi-Liang ^{[1
]}

Gu, Lian-Quan ^{[1
]}

Xu, Jun ^{[1
]}

Huang, Zhi-Shu ^{[1
]}

机构：

[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China

[2] Guangxi Univ Chinese Med, Sch Pharmaceut Sci, Nanning 530001, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 66卷

基金：

高等学校博士学科点专项科研基金;

关键词：

Isoliquiritigenin derivatives; Anti-Alzheimer agent; Amyloid-beta aggregation; 5-Lipoxygenase; Inhibitors; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; ALZHEIMERS-DISEASE; MOUSE MODEL; IN-VITRO; A-BETA; PLAQUES; CONSTITUENTS; INVOLVEMENT; EXPRESSION; PHENOTYPE;

D O I：

10.1016/j.ejmech.2013.05.015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new isoliquiritigenin (ISL) derivatives were synthesized and evaluated as dual inhibitors for amyloid-beta (A beta) aggregation and 5-lipoxygenase (5-LO). It was found that all these synthetic compounds inhibited A beta (1-42) aggregation effectively with their IC50 values ranged from 2.2 +/- 1.5 mu M to 23.8 +/- 2.0 mu M. These derivatives also showed inhibitory activity to 5-LO with their IC50 values ranged from 6.1 +/- 0.1 mu M to 35.9 +/- 0.3 mu M. Their structure activity relationships (SAR) and mechanisms of inhibitions were studied. This study provided potentially important information for further development of ISL derivatives as multifunctional agents for Alzheimer's disease (AD) treatment. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：22 / 31

页数：10

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