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.

译文

:设计,合成和评估了一系列新型白藜芦醇衍生物,作为治疗阿尔茨海默氏病的潜在治疗剂。在这些化合物中,化合物7l,(E)-5-(4-(异丙基氨基)苯乙烯基)苯-1,3-二醇表现出强力的β-淀粉样蛋白聚集抑制活性,这可通过ThT荧光测定法证实(71.65%在20μM)和透射电子显微镜(TEM)。化合物7-1也表现出良好的抗氧化活性(在氧自由基吸收能力测定中为4.12 Trolox当量,并且在10μM下细胞中的活性氧减少了37%)。化合物7f,7i,7j和7l的细胞毒性分析表明,在60μM浓度下,这些化合物的毒性低于白藜芦醇。

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