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

descriptionPublicationkeyboard_double_arrow_right Article 01 Apr 2011 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 21, pages 2,183-2,187 (issn: 0960-894X,

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

doi: 10.1016/j.bmcl.2011.03.023

pmid: 21441028

handle: 10261/49545

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

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Abstract

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.

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Keywords

Amyloid, Amyloid beta-Peptides, Quinones, BACE1, Alzheimer Disease, Aspartic Acid Endopeptidases, Humans, Ab fibrils, Amyloid Precursor Protein Secretases, Enzyme Inhibitors, Alzheimer’s disease, Amyloid aggregation

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