Design, synthesis, and evaluation of resveratrol derivatives as Aß1-42 aggregation inhibitors, antioxidants, and neuroprotective agents

作者：Lu C.; Guo Y.; Li J.; Yao M.; Liao Q.; Xie Z.; Li X.

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(24): 7683-7687.

• Aß aggregation
• Alzheimer's disease
• Antioxidant
• Neuroprotective
• Resveratrol derivatives

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 ß-amyloid aggregation inhibition activity, which was confirmed by a ThT fluorescence assay (71.65 at 20 μM) 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 μM). The cytotoxicity analysis of compounds 7f, 7i, 7j and 7l indicated that these compounds have lower toxicities than resveratrol at 60 μM.

• 出版日期2012
• 单位中山大学