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 β-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 β-amyloid peptides: Aβ1-42 and the truncated AβpE3-42.

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

Chiara Lambruschini;Denise Galante;Lisa Moni;Renata Riva;Luca Banfi;
2017

Abstract

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 β-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 β-amyloid peptides: Aβ1-42 and the truncated AβpE3-42.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11567/887532
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