4.5 Article

Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 2, Pages 426-429

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.11.068

Keywords

Boronic acids; beta-Amyloid fibrillogenesis; Glutathione; Lipid peroxidation; Caspase

Funding

  1. Ministerio de Economa y Competitividad from the government of Spain [CTQ2010-6170]
  2. Fundacion Folch for a pre-dctoral grant

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Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the beta-amyloid (beta A) aggregation process, beta-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids. (C) 2012 Elsevier Ltd. All rights reserved.

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