Multicomponent, Fragment-Based, Synthesis of Polyphenol-containing Peptidomimetics and their Inhibiting Activity on Beta Amyloid Oligomerization

A new and concise 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 the capacity to inhibit \u3b2-amyloid protein aggregation, as a possible strategy to develop new chemical entities to be used as a prevention or a therapy for Alzheimer's disease. Some of the members of the library have demonstrated, in Thioflavin assays, a highly promising activity in inhibiting aggregation for two \u3b2-amyloid peptides: A\u3b21-42 and the truncated A\u3b2pE3-42