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Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/114908
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dc.contributor.authorGarcía, Ana M.-
dc.contributor.authorBrea, José Manuel-
dc.contributor.authorMorales-García, José A.-
dc.contributor.authorPérez, Daniel I.-
dc.contributor.authorGonzález, Alejandro-
dc.contributor.authorAlonso-Gil, Sandra-
dc.contributor.authorConde, Santiago-
dc.contributor.authorCadavid, María Isabel-
dc.contributor.authorLoza, María Isabel-
dc.contributor.authorPérez Castillo, Ana-
dc.contributor.authorMartínez Gil, Ana-
dc.contributor.authorGil, Carmen-
dc.date.accessioned2015-05-08T09:17:36Z-
dc.date.available2015-05-08T09:17:36Z-
dc.date.issued2014-
dc.identifierdoi: 10.1021/jm501090m-
dc.identifierissn: 0022-2623-
dc.identifiere-issn: 1520-4804-
dc.identifier.citationJournal of Medicinal Chemistry 57(20): 8590-8607 (2014)-
dc.identifier.urihttp://hdl.handle.net/10261/114908-
dc.descriptionet al.-
dc.description.abstractA forward chemical genetic approach was followed to discover new targets and lead compounds for Parkinson's disease (PD) treatment. By analysis of the cell protection produced by some small molecules, a diphenyl sulfide compound was revealed to be a new phosphodiesterase 7 (PDE7) inhibitor and identified as a new hit. This result allows us to confirm the utility of PDE7 inhibitors as a potential pharmacological treatment of PD. On the basis of these data, a diverse family of diphenyl sulfides has been developed and pharmacologically evaluated in the present work. Moreover, to gain insight into the safety of PDE7 inhibitors for human chronic treatment, we evaluated the new compounds in a surrogate emesis model, showing nonemetic effects.-
dc.description.sponsorshipFinancial support from MINECO and FEDER founds (UE program) (project nos. IPT-2012-0762-300000 and SAF2012-33600) and MICINN (SAF2010-15793 to O.V. and SAF2010-16365 to A.P.-C.) are acknowledged. A.M.G. and D. I. P. acknowledge a predoctoral and postdoctoral grants respectively to the CSIC (JAE program). CIBERNED is funded by the Instituto de Salud Carlos III. J.A.M-G. is a fellow from CIBERNED. BRAINco Biopharma SL reviewed and funded the pro-emetic studies of rolipram, roflumilast, BRL50481, VP1.15, and TC3.6 compounds.-
dc.publisherAmerican Chemical Society-
dc.rightsclosedAccess-
dc.titleModulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors-
dc.typeartículo-
dc.identifier.doi10.1021/jm501090m-
dc.date.updated2015-05-08T09:17:36Z-
dc.description.versionPeer Reviewed-
dc.language.rfc3066eng-
dc.contributor.funderMinisterio de Economía y Competitividad (España)-
dc.contributor.funderMinisterio de Ciencia e Innovación (España)-
dc.contributor.funderEuropean Commission-
dc.contributor.funderConsejo Superior de Investigaciones Científicas (España)-
dc.contributor.funderCentro Investigación Biomédica en Red Enfermedades Neurodegenerativas (España)-
dc.contributor.funderInstituto de Salud Carlos III-
dc.contributor.funderBRAINco Biopharma-
dc.relation.csicSí-
dc.identifier.funderhttp://dx.doi.org/10.13039/501100003329es_ES
dc.identifier.funderhttp://dx.doi.org/10.13039/501100004837es_ES
dc.identifier.funderhttp://dx.doi.org/10.13039/501100000780es_ES
dc.identifier.funderhttp://dx.doi.org/10.13039/501100003339es_ES
dc.identifier.funderhttp://dx.doi.org/10.13039/501100004587es_ES
dc.type.coarhttp://purl.org/coar/resource_type/c_6501es_ES
item.openairetypeartículo-
item.cerifentitytypePublications-
item.grantfulltextnone-
item.fulltextNo Fulltext-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
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