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

Bioorg Med Chem Lett. 2013 Jan 15;23(2):426-9. doi: 10.1016/j.bmcl.2012.11.068. Epub 2012 Nov 29.

Abstract

Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemical synthesis*
  • Alkenes / chemistry
  • Alkenes / pharmacology
  • Alzheimer Disease / drug therapy*
  • Apoptosis / drug effects*
  • Boronic Acids / chemical synthesis*
  • Boronic Acids / chemistry
  • Boronic Acids / pharmacology
  • Cell Line, Tumor
  • Drug Delivery Systems
  • Drug Discovery*
  • Humans
  • Models, Biological
  • Neuroprotective Agents / chemical synthesis*
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / pharmacology

Substances

  • Alkenes
  • Boronic Acids
  • Neuroprotective Agents