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http://hdl.handle.net/10261/112415
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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Benchekroun, Mohamed | es_ES |
dc.contributor.author | Bartolini, Manuela | es_ES |
dc.contributor.author | Egea, Javier | es_ES |
dc.contributor.author | Romero Jódar, Alejandro | es_ES |
dc.contributor.author | Soriano, Elena | es_ES |
dc.contributor.author | Pudlo, M. | es_ES |
dc.contributor.author | Luzet, Vincenza | es_ES |
dc.contributor.author | Andrisano, V. | es_ES |
dc.contributor.author | Jimeno, M. Luisa | es_ES |
dc.contributor.author | López, M. G. | es_ES |
dc.contributor.author | Wehle, S. | es_ES |
dc.contributor.author | Gharbi, T. | es_ES |
dc.contributor.author | Refouvelet, B. | es_ES |
dc.contributor.author | Andrés, Lucía de | es_ES |
dc.contributor.author | Herrera-Arozamena, Clara | es_ES |
dc.contributor.author | Monti, B. | es_ES |
dc.contributor.author | Bolognesi, Maria Laura | es_ES |
dc.contributor.author | Rodríguez-Franco, María Isabel | es_ES |
dc.contributor.author | Decker, Michael | es_ES |
dc.contributor.author | Marco-Contelles, José | es_ES |
dc.contributor.author | Ismaili, L. | es_ES |
dc.date.issued | 2015 | - |
dc.identifier | doi: 10.1002/cmdc.201402409 | - |
dc.identifier | issn: 1860-7187 | - |
dc.identifier | e-issn: 1860-7187 | - |
dc.identifier.citation | ChemMedChem 10: 523-539 (2015) | es_ES |
dc.identifier.uri | http://hdl.handle.net/10261/112415 | - |
dc.description.abstract | Herein we describe the design, multicomponent synthesis, and biological, molecular modeling and ADMET studies, as well as in vitro PAMPA-blood-brain barrier (BBB) analysis of new tacrine-ferulic acid hybrids (TFAHs). We identified (E)-3-(hydroxy-3-methoxyphenyl)-N-{8[(7-methoxy-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl}-N-[2-(naphthalen-2-ylamino)2-oxoethyl]acrylamide (TFAH 10n) as a particularly interesting multipotent compound that shows moderate and completely selective inhibition of human butyrylcholinesterase (IC50 = 68.2 nm ), strong antioxidant activity (4.29 equiv trolox in an oxygen radical absorbance capacity (ORAC) assay), and good β-amyloid (Aβ) anti-aggregation properties (65.6% at 1:1 ratio); moreover, it is able to permeate central nervous system (CNS) tissues, as determined by PAMPA-BBB assay. Notably, even when tested at very high concentrations, TFAH 10n easily surpasses the other TFAHs in hepatotoxicity profiling (59.4% cell viability at 1000 μm), affording good neuroprotection against toxic insults such as Aβ1-40, Aβ1-42, H2O2, and oligomycin A/rotenone on SH-SY5Y cells, at 1 μm. The results reported herein support the development of new multipotent TFAH derivatives as potential drugs for the treatment of Alzheimer's disease. | - |
dc.publisher | Wiley-VCH | es_ES |
dc.relation.isversionof | Preprint | - |
dc.rights | openAccess | - |
dc.subject | Inhibitors | - |
dc.subject | Cholinesterases | - |
dc.subject | Multicomponent reactions | - |
dc.subject | Neuroprotection | - |
dc.subject | Antioxidants | - |
dc.subject | Alzheimer’s disease | - |
dc.title | Novel tacrine-grafted ugi adducts as multipotent anti-alzheimer drugs: A synthetic renewal in tacrine-ferulic acid hybrids | es_ES |
dc.type | artículo | es_ES |
dc.identifier.doi | 10.1002/cmdc.201402409 | - |
dc.date.updated | 2015-03-16T11:30:14Z | - |
dc.description.version | Peer Reviewed | - |
dc.language.rfc3066 | eng | - |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (España) | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | - |
dc.relation.csic | Sí | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003339 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | With Fulltext | - |
item.cerifentitytype | Publications | - |
item.openairetype | artículo | - |
item.grantfulltext | open | - |
Aparece en las colecciones: | (CENQUIOR) Artículos (IQM) Artículos (IQOG) Artículos |
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Novel Tacrine-Grafted Ugi Adducts.pdf | 1,01 MB | Adobe PDF | Visualizar/Abrir |
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