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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | González Muñoz, Gema C. | - |
dc.contributor.author | Arce, Mariana P. | - |
dc.contributor.author | López, Beatriz | - |
dc.contributor.author | Pérez, Concepción | - |
dc.contributor.author | Villarroya, Mercedes | - |
dc.contributor.author | López, Manuela G. | - |
dc.contributor.author | García, Antonio G. | - |
dc.contributor.author | Conde, Santiago | - |
dc.contributor.author | Rodríguez-Franco, María Isabel | - |
dc.date.accessioned | 2011-06-06T11:48:58Z | - |
dc.date.available | 2011-06-06T11:48:58Z | - |
dc.date.issued | 2010 | - |
dc.identifier.citation | European Journal of Medicinal Chemistry 45 : 6152-6158 | es_ES |
dc.identifier.uri | http://hdl.handle.net/10261/36539 | - |
dc.description.abstract | From an in-house library of compounds, five phenothiazines and one dibenzothiadiazepine were selected to be tested in neuroprotective and cholinergic assays. Three of them, derived from the N-alkylphenothiazine, the N-acylaminophenothiazine, and the 1,4,5-dibenzo[b,f]thiadiazepine system, protected human neuroblastoma cells against oxidative stress generated by both exogenous and mitochondrial free radicals. They could also penetrate the CNS, according to an in vitro bloodebrain barrier model, and an N-acylaminophenothiazine derivative behaved as a selective inhibitor of butyrylcholinesterase. Free radical capture and/or promotion of antioxidant protein biosynthesis are mechanisms that can be implicated in their neuroprotective actions. Due to their excellent pharmacological properties and the fact that they were not biologically explored in the past, one N-acylaminophenothiazine and one 1,4,5-dibenzo[b,f]thiadiazepine have been selected to develop two new series that are currently in progress | es_ES |
dc.description.sponsorship | This work is dedicated to our dear colleagues Prof. Carlos Corral (deceased) and Dr. Jaime Lissavetzky, which conducted the first syntheses of these compounds. The authors gratefully acknowledge the financial support of Spanish Ministry of Science and Innovation MICINN (projects SAF2006-01249, SAF2009-13015-C02-01, and SAF2009-12150), Community of Madrid (Programa de Actividades de I þ D entre Grupos de Investigación en Biociencias, project S-SAL/0275/2006), and the Institute of Health Carlos III (Red RENEVAS, RETICS-RD06/0026). The fellowships to G.C.G.-M. and M.P.A. from CSIC and MICINN respectively, are also acknowledged. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | Elsevier | es_ES |
dc.rights | closedAccess | es_ES |
dc.subject | Phenothiazines | es_ES |
dc.subject | Dibenzothiadiazepines | es_ES |
dc.subject | Dibenzothiadiazepines | es_ES |
dc.subject | Neuroprotection | es_ES |
dc.subject | Oxidative stress | es_ES |
dc.subject | Butyrylcholinesterase inhibition | es_ES |
dc.title | Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow’s neuroprotective therapies against neurodegenerative diseases | es_ES |
dc.type | artículo | es_ES |
dc.identifier.doi | 10.1016/j.ejmech.2010.09.039 | | - |
dc.description.peerreviewed | Peer reviewed | es_ES |
dc.relation.publisherversion | http://dx.doi.org/10.1016/j.ejmech.2010.09.039 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | none | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | No Fulltext | - |
item.languageiso639-1 | en | - |
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