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

2016; Frontiers Media; Volume: 10; Linguagem: Inglês

10.3389/fnins.2016.00294

1662-4548

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

Computational Drug Discovery Methods

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 showing antioxidant, anti-beta-amyloid, anti-inflammatory, as well as cholinesterase and monoamine oxidase 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, possessing antioxidant and neuroprotective properties.