A new and short fragment-based approach towards artificial (but “natural-based”) complex polyphenols has been developed, exploiting the Ugi multicomponent reaction of phenol-containing simple substrates. The resulting library of compounds has been tested for its capacity to inhibit β-amyloid protein aggregation, as a possible strategy to develop new chemical entities to be used as prevention or therapy for Alzheimer's disease. Some of the members of this library have demonstrated, in thioflavin assays, a highly promising activity in inhibiting aggregation for two β-amyloid peptides: Aβ1-42 and the truncated AβpE3-42.

中文翻译：

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多组分，基于片段的多酚类肽模拟物的合成及其对β-淀粉样蛋白低聚的抑制活性

利用含酚的简单底物的Ugi多组分反应，已经开发了一种新的基于短片段的人工（但基于“天然”）复杂多酚的方法。已经测试了所得化合物库抑制β淀粉样蛋白聚集的能力，这是开发新的化学实体以用作预防或治疗阿尔茨海默氏病的可能策略。该库的某些成员在硫黄素分析中证明了在抑制两个β淀粉样肽：Aβ1-42和截短的AβpE3-42聚集方面具有非常有前途的活性。