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

José Marco-Contelles; Mercedes Unzeta; Gerard Esteban; Rona Ramsay; Alejandro Romero; Ricardo Martínez-Murillo; Maria C. Carreiras; Lhassane Ismaili; Irene Bolea

doi:10.3389/fnins.2016.00294

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

José Marco-Contelles, Mercedes Unzeta, Gerard Esteban, Rona Ramsay, Alejandro Romero, Ricardo Martínez-Murillo, Maria C. Carreiras, Lhassane Ismaili, Irene Bolea

Research output: Contribution to journal › Review article › peer-review

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.

Original language	English
Article number	294
Number of pages	7
Journal	Frontiers in Neuroscience
Volume	10
DOIs	https://doi.org/10.3389/fnins.2016.00294
Publication status	Published - 28 Jun 2016

Keywords

Multi-target directed ligands,
Alzheimer’s disease
Monomaine oxidases
Cholinesterases
Drugs

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10.3389/fnins.2016.00294Licence: CC BY

Ramsay_2016_FN_ASS234_CC
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.
Final published version, 419 KBLicence: CC BY

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@article{0d6a6aed4e114942ad84825d8a1eb309,

title = "ASS234, as a new Multi-Target Directed propargylamine for Alzheimer{\textquoteright}s disease therapy",

abstract = "The complex nature of Alzheimer{\textquoteright}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.",

keywords = "Multi-target directed ligands,, Alzheimer{\textquoteright}s disease, Monomaine oxidases, Cholinesterases, Drugs",

author = "Jos{\'e} Marco-Contelles and Mercedes Unzeta and Gerard Esteban and Rona Ramsay and Alejandro Romero and Ricardo Mart{\'i}nez-Murillo and Carreiras, \{Maria C.\} and Lhassane Ismaili and Irene Bolea",

note = "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.",

year = "2016",

month = jun,

day = "28",

doi = "10.3389/fnins.2016.00294",

language = "English",

volume = "10",

journal = "Frontiers in Neuroscience",

issn = "1662-453X",

publisher = "Frontiers Media S. A.",

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TY - JOUR

T1 - ASS234, as a new Multi-Target Directed propargylamine for Alzheimer’s disease therapy

AU - Marco-Contelles, José

AU - Unzeta, Mercedes

AU - Esteban, Gerard

AU - Ramsay, Rona

AU - Romero, Alejandro

AU - Martínez-Murillo, Ricardo

AU - Carreiras, Maria C.

AU - Ismaili, Lhassane

AU - Bolea, Irene

N1 - 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.

PY - 2016/6/28

Y1 - 2016/6/28

N2 - 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.

AB - 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.

KW - Multi-target directed ligands,

KW - Alzheimer’s disease

KW - Monomaine oxidases

KW - Cholinesterases

KW - Drugs

UR - https://www.scopus.com/pages/publications/84980396145

U2 - 10.3389/fnins.2016.00294

DO - 10.3389/fnins.2016.00294

M3 - Review article

SN - 1662-453X

VL - 10

JO - Frontiers in Neuroscience

JF - Frontiers in Neuroscience

M1 - 294

ER -

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

Abstract

Keywords

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COST Application: COST CM21103-CGA-I

Cite this

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

Abstract

Keywords

Access to Document

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Projects

COST Application: COST CM21103-CGA-I

Cite this