Multicomponent, fragment-based synthesis of polyphenol-containing peptidomimetics and their inhibiting activity on beta-amyloid oligomerization
| Autor: | Denise Galante, Alessia Traverso, Giulio Gancia, Luca Banfi, Cristina D'Arrigo, Renata Riva, Lisa Moni, Chiara Lambruschini, Francesco Ferraro |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
multicomponent reaction
Amyloid Peptidomimetic Protein aggregation 010402 general chemistry 01 natural sciences Biochemistry beta-amyloids chemistry.chemical_compound Protein structure Fragment (logic) Physical and Theoretical Chemistry Beta (finance) Protein Structure Quaternary Amyloid beta-Peptides 010405 organic chemistry Chemistry Organic Chemistry Polyphenols Combinatorial chemistry Peptide Fragments 0104 chemical sciences Kinetics Polyphenol peptidomimetics alzheimer's disease Thioflavin Protein Multimerization polyphenols of synthesis |
| Zdroj: | Organic & biomolecular chemistry 15 (2017): 9331–9351. doi:10.1039/c7ob02182h info:cnr-pdr/source/autori:Lambruschini, Chiara; Galante, Denise; Moni, Lisa; Ferraro, Francesco; Gancia, Giulio; Riva, Renata; Traverso, Alessia; Banfi, Luca; D'Arrigo, Cristina/titolo:Multicomponent, fragment-based synthesis of polyphenol-containing peptidomimetics and their inhibiting activity on beta-amyloid oligomerization/doi:10.1039%2Fc7ob02182h/rivista:Organic & biomolecular chemistry/anno:2017/pagina_da:9331/pagina_a:9351/intervallo_pagine:9331–9351/volume:15 |
| DOI: | 10.1039/c7ob02182h |
| Popis: | 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 beta-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 beta-amyloid peptides: A beta 1-42 and the truncated A beta pE3-42. |
| Databáze: | OpenAIRE |
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