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dc.contributor.authorPineda de las Infantas y Villatoro, María J.
dc.contributor.authorUnciti-Broceta, Juan Diego
dc.contributor.authorContreras-Montoya, Rafael
dc.contributor.authorGarcía-Salcedo, José Antonio
dc.contributor.authorGallo Mezo, Miguel Ángel 
dc.contributor.authorUnciti-Broceta, Asier
dc.contributor.authorDíaz-Mochón, Juan J.
dc.date.accessioned2015-04-10T07:14:51Z
dc.date.available2015-04-10T07:14:51Z
dc.date.issued2015
dc.identifier.citationPineda de las Infantas y Villatoro, M.J.; et al. Amide-controlled, one-pot synthesis of tri-substituted purines generates structural diversity and analogues with trypanocidal activity. Scientific Reports, 5: 9139 (2015). [http://hdl.handle.net/10481/35509]es_ES
dc.identifier.issn2045-2322
dc.identifier.urihttp://hdl.handle.net/10481/35509
dc.description.abstractAnovel one-pot synthesis of tri-substituted purines and the discovery of purine analogues with trypanocidal activity are reported. The reaction is initiated by a metal-free oxidative coupling of primary alkoxides and diaminopyrimidines with Schiff base formation and subsequent annulation in the presence of large N,N-dimethylamides (e.g.N,N-dimethylpropanamide or larger). This synthetic route is in competition with a reaction previously-reported by our group1, allowing the generation of a combinatorial library of tri-substituted purines by the simple modification of the amide and the alkoxide employed. Among the variety of structures generated, two purine analogues displayed trypanocidal activity against the protozoan parasite Trypanosoma brucei with IC50 , 5 mM, being each of those compounds obtained through each of the synthetic pathways.es_ES
dc.description.sponsorshipJ.J.D.M. thanks Spanish Ministerio de Economı´a y Competitividad for a Ramon y Cajal Fellowship. A.U.B. thanks MRC IGMM for an academic fellowship. This work was partially supported by Grant SAF2011-30528 to J.A.G.S..es_ES
dc.language.isoenges_ES
dc.publisherNature Publishing Groupes_ES
dc.rightsCreative Commons Attribution-NonCommercial-NoDerivs 3.0 Licensees_ES
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/3.0/es_ES
dc.subjectReaction mechanismses_ES
dc.subjectParasite biologyes_ES
dc.subjectPurineses_ES
dc.subjectTrypanosoma bruceies_ES
dc.subjectTrypanocidal activityes_ES
dc.titleAmide-controlled, one-pot synthesis of tri-substituted purines generates structural diversity and analogues with trypanocidal activityes_ES
dc.typeinfo:eu-repo/semantics/articlees_ES
dc.rights.accessRightsinfo:eu-repo/semantics/openAccesses_ES
dc.identifier.doi10.1038/srep09139


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