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Título: | ASS234, As a New Multi-Target Directed Propargylamine for Alzheimer's Disease Therapy |
Autor: | Marco-Contelles, José CSIC ORCID; Unzeta, Mercedes; Bolea, Irene; Esteban, Gerard; Ramsay, Rona R.; Romero Jódar, Alejandro CSIC ORCID; Martínez-Murillo, Ricardo CSIC ORCID; Carreiras, M. Carmo; Ismaili, L. | Fecha de publicación: | 28-jun-2016 | Editor: | Frontiers Media | Citación: | Frontiers in Neuroscience 10: 294 (2016) | Resumen: | Highlights:ASS2324 is a hybrid compound resulting from the juxtaposition of donepezil and the propargylamine PF9601NASS2324 is a multi-target directed propargylamine able to bind to all the AChE/BuChE and MAO A/B enzymesASS2324 shows antioxidant, neuroprotective and suitable permeability propertiesASS2324 restores the scopolamine-induced cognitive impairment to the same extent as donepezil, and is less toxicASS2324 prevents β-amyloid induced aggregation in the cortex of double transgenic miceASS2324 is the most advanced anti-Alzheimer agent for pre-clinical studies that we have identified in our laboratoriesThe 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 Aβ-aggregation, and possessing antioxidant and neuroprotective properties. | Versión del editor: | http://dx.doi.org/10.3389/fnins.2016.00294 | URI: | http://hdl.handle.net/10261/152978 | DOI: | 10.3389/fnins.2016.00294 | ISSN: | 1662-4548 |
Aparece en las colecciones: | (IQOG) Artículos (IC) Artículos |
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ASS234 As a New Multi-Target Directed.pdf | 615,39 kB | Adobe PDF | Visualizar/Abrir |
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