ASS234, as a new Multi-Target Directed propargylamine for Alzheimer’s disease therapy
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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-betaamyloid, 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.
Marco-Contelles , J , Unzeta , M , Esteban , G , Ramsay , R , Romero , A , Martínez-Murillo , R , Carreiras , M C , Ismaili , L & Bolea , I 2016 , ' ASS234, as a new Multi-Target Directed propargylamine for Alzheimer’s disease therapy ' Frontiers in Neuroscience , vol 10 , 294 . DOI: 10.3389/fnins.2016.00294
Frontiers in Neuroscience
Copyright © 2016 Marco-Contelles, Unzeta, Bolea, Esteban, Ramsay, Romero, Martínez-Murillo, Carreiras and Ismaili. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
MU and JMC thank MINECO (Spain) for support (Grant SAF2012-33304; SAF2015-65586-R). RRR, MU, GE and JMC thank EU (COST Action 1103) for support.
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