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

…, KL Jiménez-Aliaga, P Bermejo-Bescós…

Index: Ortega, Andrea; Rincon, Angela; Jimenez-Aliaga, Karim L.; Bermejo-Bescos, Paloma; Martin-Aragon, Sagrario; Molina, Maria Teresa; Csaky, Aurelio G. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2183 - 2187

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Citation Number: 25

Abstract

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, ...