Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/172618
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DC Field | Value | Language |
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dc.contributor.author | Abás Prades, Sònia | - |
dc.contributor.author | Rodríguez-Arévalo, Sergio | - |
dc.contributor.author | Bagan Polonio, Andrea | - |
dc.contributor.author | Griñán Ferré, Christian | - |
dc.contributor.author | Vasilopoulou, Foteini | - |
dc.contributor.author | Brocos-Mosquera, Iria | - |
dc.contributor.author | Muguruza, Carolina | - |
dc.contributor.author | Pérez, Belén | - |
dc.contributor.author | Molins i Grau, Elies | - |
dc.contributor.author | Luque Garriga, F. Xavier | - |
dc.contributor.author | Pérez Lozano, Pilar | - |
dc.contributor.author | Jonghe, Steven de | - |
dc.contributor.author | Daelemans, Dirk | - |
dc.contributor.author | Naesens, Lieve | - |
dc.contributor.author | Brea, José | - |
dc.contributor.author | Loza, María Isabel | - |
dc.contributor.author | Hernández-Hernández, Elena | - |
dc.contributor.author | García-Sevilla, Jesús A. | - |
dc.contributor.author | García-Fuster, M. Julia | - |
dc.contributor.author | Radan, Milica | - |
dc.contributor.author | Djikic, Teodora | - |
dc.contributor.author | Nikolic, Katarina | - |
dc.contributor.author | Pallàs i Llibería, Mercè, 1964- | - |
dc.contributor.author | Callado, Luis F. | - |
dc.contributor.author | Escolano Mirón, Carmen | - |
dc.date.accessioned | 2020-12-10T11:51:58Z | - |
dc.date.available | 2021-03-19T06:10:23Z | - |
dc.date.issued | 2020-03-19 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/2445/172618 | - |
dc.description.abstract | Imidazoline I2 receptors (I2-IR), widely distributed in the CNS and altered in patients that suffered from neurodegenerative disorders, are orphan from the structural point of view and new I2-IR ligands are urgently required for improving their pharmacological characterization. We report the synthesis and 3D-QSAR studies of a new family of bicyclic α-iminophosphonates endowed with relevant affinities for human brain I2-IR. Acute treatment in mice with a selected compound significantly decreased the FADD protein in the hippocampus, a key marker in neuroprotective actions. Additionally, in vivo studies in the familial Alzheimer's disease 5xFAD murine model revealed beneficial effects in behavior and cognition. These results are supported by changes in molecular pathways related to cognitive decline and Alzheimer's disease. Therefore bicyclic α-iminophosphonates are tools that may open new therapeutic avenues for I2-IR, particularly for unmet neurodegenerative conditions. | - |
dc.format.extent | 24 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Versió postprint del document publicat a: https://doi.org/10.1021/acs.jmedchem.9b02080 | - |
dc.relation.ispartof | Journal of Medicinal Chemistry, 2020, vol. 63, p. 3610-3633 | - |
dc.relation.uri | https://doi.org/10.1021/acs.jmedchem.9b02080 | - |
dc.rights | (c) American Chemical Society , 2020 | - |
dc.source | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) | - |
dc.subject.classification | Malaltia d'Alzheimer | - |
dc.subject.classification | Malalties neurodegeneratives | - |
dc.subject.classification | Envelliment | - |
dc.subject.other | Alzheimer's disease | - |
dc.subject.other | Neurodegenerative Diseases | - |
dc.subject.other | Aging | - |
dc.title | Bicyclic alfa-iminophosphonates as high affinity imidazoline I2 receptor ligands for Alzheimer's disease | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 700177 | - |
dc.date.updated | 2020-12-10T11:51:59Z | - |
dc.relation.projectID | info:eu-repo/grantAgreement/EC/H2020/747487/EU//Schizo-EPICOG | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia) Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica) |
Files in This Item:
File | Description | Size | Format | |
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700177.pdf | 2.7 MB | Adobe PDF | View/Open |
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