Synthesis and evaluation of arylquinones as BACE1 inhibitors, β-amyloid peptide aggregation inhibitors, and destabilizers of preformed β-amyloid fibrils

Andrea Ortega, Ángela Rincón, Karim L. Jiménez-Aliaga, Paloma Bermejo-Bescós, Sagrario Martín-Aragón, María Teresa Molina, Aurelio G. Csákÿ

Resultado de la investigación: Contribución a una revistaArtículorevisión exhaustiva

27 Citas (Scopus)

Resumen

BACE1 activity, inhibition of Aβ aggregation, and disaggregation of preformed Aβ fibrils constitute the three major targets in the development of small-molecule lipophilic new drugs for the treatment of Alzheimer's disease (AD). Quinones are widely distributed among natural products and possess relevant and varied biological activities including antitumor and antibiotic, inhibition of HIV-1 reverse transcriptase, antidiabetic, or COX-inhibition, among others. We report herein the interaction of several arylquinones and their derivatives with the amyloidogenic pathway of the amyloid precursor protein processing. Our studies put forward that these compounds are promising candidates in the development of new drugs which are effective simultaneously towards the three major targets of AD.

Idioma originalInglés
Páginas (desde-hasta)2183-2187
Número de páginas5
PublicaciónBioorganic and Medicinal Chemistry Letters
Volumen21
N.º8
DOI
EstadoPublicada - 15 abr 2011

Nota bibliográfica

Copyright:
Copyright 2011 Elsevier B.V., All rights reserved.

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