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Issue 44, 2017
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Multicomponent, fragment-based synthesis of polyphenol-containing peptidomimetics and their inhibiting activity on beta-amyloid oligomerization

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Abstract

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.

Graphical abstract: Multicomponent, fragment-based synthesis of polyphenol-containing peptidomimetics and their inhibiting activity on beta-amyloid oligomerization

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Publication details

The article was received on 31 Aug 2017, accepted on 23 Oct 2017 and first published on 23 Oct 2017


Article type: Paper
DOI: 10.1039/C7OB02182H
Citation: Org. Biomol. Chem., 2017,15, 9331-9351
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    Multicomponent, fragment-based synthesis of polyphenol-containing peptidomimetics and their inhibiting activity on beta-amyloid oligomerization

    C. Lambruschini, D. Galante, L. Moni, F. Ferraro, G. Gancia, R. Riva, A. Traverso, L. Banfi and C. D'Arrigo, Org. Biomol. Chem., 2017, 15, 9331
    DOI: 10.1039/C7OB02182H

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