ASS234, As a New Multi-Target Directed Propargylamine for Alzheimer's Disease Therapy

Highlights: 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...

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Detalles Bibliográficos
Autores: Marco-Contelles, José, Unzeta López, Mercedes|||0000-0002-7113-3383, Bolea Tomás, Irene|||0000-0001-9591-980X, Esteban, Gerard|||0000-0002-9383-2150, Ramsay, Rona R., Romero, Alejandro|||0000-0001-5483-4973, Martínez-Murillo, Ricard, Carreiras, M. Carmo, Ismaili, Lhassane
Tipo de recurso: artículo
Fecha de publicación:2016
País:España
Institución:Universitat Autònoma de Barcelona
Repositorio:Dipòsit Digital de Documents de la UAB
Idioma:inglés
OAI Identifier:oai:ddd.uab.cat:254185
Acceso en línea:https://ddd.uab.cat/record/254185
https://dx.doi.org/urn:doi:10.3389/fnins.2016.00294
Access Level:acceso abierto
Palabra clave:Multi-target directed ligands
Alzheimer's disease
Monoamine oxidases
Cholinesterases
Drugs
Descripción
Sumario:Highlights: 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 Aβ-aggregation, and possessing antioxidant and neuroprotective properties.

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