二芳基γ-二氢吡喃酮衍生物的设计、合成与评价：作为环姜黄素类似物和淀粉样 β 聚集抑制剂。
Design, synthesis and evaluation of diaryl γ-dihydropyrone derivatives as cyclocurcumin mimetics and inhibitors of the aggregation of amyloid β.
机构信息
Department of Biochemical Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
Department of Biochemical Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
出版信息
Bioorg Chem. 2020 Nov;104:104302. doi: 10.1016/j.bioorg.2020.104302. Epub 2020 Sep 22.
A structure activity relationship study of cyclocurcumin-derived, diaryl γ-dihydropyrone-based inhibitors of amyloid β aggregation is described. Optimization of the diaryl γ-dihydropyrone framework and two phenolic rings resulted in the identification of diaryl γ-dihydropyrone type cyclocurcumin analogue AY1511, which exhibited potent anti-amyloid β aggregation activity (leading to nanorod-like fragments), sufficient water solubility, and low cytotoxicity.
描述了一类基于环荞麦素衍生的二芳基γ-二氢吡喃酮的淀粉样β聚集抑制剂的构效关系研究。对二芳基γ-二氢吡喃酮骨架和两个酚环进行优化，得到了二芳基γ-二氢吡喃酮型环荞麦素类似物 AY1511，其表现出很强的抗淀粉样β聚集活性（导致纳米棒状片段）、足够的水溶性和低细胞毒性。
Zotero 插件