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ASS234, as a new Multi-Target Directed propargylamine for Alzheimer’s disease therapy

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Ramsay_2016_FN_ASS234_CC.pdf (418.6Kb)
Date
28/06/2016
Author
Marco-Contelles, José
Unzeta, Mercedes
Esteban, Gerard
Ramsay, Rona
Romero, Alejandro
Martínez-Murillo, Ricardo
Carreiras, Maria C.
Ismaili, Lhassane
Bolea, Irene
Keywords
Multi-target directed ligands,
Alzheimer’s disease
Monomaine oxidases
Cholinesterases
Drugs
RC0321 Neuroscience. Biological psychiatry. Neuropsychiatry
RA Public aspects of medicine
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Abstract
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.
Citation
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 . https://doi.org/10.3389/fnins.2016.00294
Publication
Frontiers in Neuroscience
Status
Peer reviewed
DOI
https://doi.org/10.3389/fnins.2016.00294
ISSN
1662-453X
Type
Journal item
Rights
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.
Description
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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  • University of St Andrews Research
URI
http://hdl.handle.net/10023/9054

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