Design, synthesis, and evaluation of resveratrol derivatives as Aβ1-42 aggregation inhibitors, antioxidants, and neuroprotective agents

被引：46

作者：

Lu, Chuanjun ^{[1
]}

Guo, Yueyan ^{[1
]}

Li, Jianheng ^{[1
]}

Yao, Meicun ^{[1
]}

Liao, Qiongfeng ^{[2
]}

Xie, Zhiyong ^{[1
]}

Li, Xingshu ^{[1
]}

机构：

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

[2] Guangzhou Univ Tradit Chinese Med, Coll Chinese Tradit Med, Guangzhou 510006, Guangdong, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 24期

关键词：

Resveratrol derivatives; Alzheimer's disease; A beta aggregation; Antioxidant; Neuroprotective; ALZHEIMERS-DISEASE;

D O I：

10.1016/j.bmcl.2012.09.105

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel resveratrol derivatives were designed, synthesised and evaluated as potential therapeutic agents for the treatment of Alzheimer's disease. Among these compounds, compound 7l, (E)-5-(4-(isopropylamino)styryl)benzene-1,3-diol, exhibited potent beta-amyloid aggregation inhibition activity, which was confirmed by a ThT fluorescence assay (71.65% at 20 mu M) and transmission electron microscopy (TEM). Compound 7l also exhibited good antioxidant activity (4.12 Trolox equivalents in an oxygen radical absorbance capacity assay and a 37% reduction in reactive oxygen species in cells at 10 mu M). The cytotoxicity analysis of compounds 7f, 7i, 7j and 7l indicated that these compounds have lower toxicities than resveratrol at 60 mu M. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：7683 / 7687

页数：5

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