ASS234, as a new multi-target directed propargylamine for Alzheimer's disease therapy

José Marco-Contelles, Mercedes Unzeta, Irene Bolea, Gerard Esteban, Rona R. Ramsay, Alejandro Romero, Ricard Martínez-Murillo, M. Carmo Carreiras, Lhassane Ismaili

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33 Citations (Scopus)

Abstract

© 2016 Marco-Contelles, Unzeta, Bolea, Esteban, Ramsay, Romero, Martínez-Murillo, Carreiras and Ismaili. The complex nature of Alzheimer's disease (AD) has prompted the design of Multi-Target-Directed Ligands (MTDL) able to bind to diverse biochemical targets involved in the progress and development of the disease. In this context, we have designed a number of MTD propargylamines (MTDP) showing antioxidant, anti-beta-amyloid, anti-inflammatory, as well as cholinesterase and monoamine oxidase (MAO) inhibition capacities. Here, we describe these properties in the MTDL ASS234, our lead-compound ready to enter in pre-clinical studies for AD, as a new multipotent, permeable cholinesterase/monoamine oxidase inhibitor, able to inhibit Aß-aggregation, and possessing antioxidant and neuroprotective properties.
Original languageEnglish
Article number294
JournalFrontiers in Neuroscience
Volume10
Issue numberJUN
DOIs
Publication statusPublished - 28 Jun 2016

Keywords

  • Alzheimer's disease
  • Cholinesterases
  • Drugs
  • Monoamine oxidases
  • Multi-target directed ligands

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    Marco-Contelles, J., Unzeta, M., Bolea, I., Esteban, G., Ramsay, R. R., Romero, A., Martínez-Murillo, R., Carreiras, M. C., & Ismaili, L. (2016). ASS234, as a new multi-target directed propargylamine for Alzheimer's disease therapy. Frontiers in Neuroscience, 10(JUN), [294]. https://doi.org/10.3389/fnins.2016.00294