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dc.contributor.authorRetamosa Hernández, María Graciaes_ES
dc.contributor.authorDíez-Martínez, Robertoes_ES
dc.contributor.authorMaestro, Beatrizes_ES
dc.contributor.authorGarcía-Fernández, Estheres_ES
dc.contributor.authorde Waal, Bases_ES
dc.contributor.authorMeijer, E. W.es_ES
dc.contributor.authorGarcía, Pedroes_ES
dc.contributor.authorSanz, Jesús M.es_ES
dc.date.issued2015-09-17-
dc.identifier.citationAngewandte Chemie (2015)es_ES
dc.identifier.issn1433-7851-
dc.identifier.urihttp://hdl.handle.net/10261/131014-
dc.description1 schem.-2 tab.-3 fig.es_ES
dc.description.abstractA double approach was followed in the search of novel inhibitors of the surface choline-binding proteins (CBPs) of Streptococcus pneumoniae (pneumococcus) with antimicrobial properties. First, a library of 49 rationally-designed esters of alkyl amines was screened for their specific binding to CBPs. The best binders, being esters of bicyclic amines (EBAs), were then tested for their in vitro effect on pneumococcal growth and morphology. Second, the efficiency of EBA-induced CBP inhibition was enhanced about 45 000-fold by multivalency effects upon synthesizing a poly(propylene imine) dendrimer containing eight copies of an atropine derivative. Both approaches led to compounds that arrest bacterial growth, dramatically decrease cell viability, and exhibit a protection effect in animal disease models, demonstrating that the pneumococcal CBPs are adequate targets for the discovery of novel antimicrobials that overcome the currently increasing antimicrobial resistance issues.es_ES
dc.description.sponsorshipThis work was supported by grants BFU2010-17824 and BIO2013-47684-R (Spanish Ministry of Education and Science), and EU-CP223111 (CAREPNEUMO, European Union).es_ES
dc.language.isoenges_ES
dc.publisherWiley-VCHes_ES
dc.rightsopenAccesses_ES
dc.subjectPneumococcuses_ES
dc.subjectAntibiotic resistancees_ES
dc.subjectDrug designes_ES
dc.subjectCholine-binding proteinses_ES
dc.subjectDendrimerses_ES
dc.titleAromatic esters of bicyclic amines as antimicrobials against Streptococcus pneumoniaees_ES
dc.title.alternativeAromatic esters of bicyclic amines: a new generation of antimicrobials against Streptococcus pneumoniaees_ES
dc.typeArtículoes_ES
dc.identifier.doi10.1002/ange.201505700-
dc.description.peerreviewedNoes_ES
dc.relation.publisherversionhttp://dx.doi.org/ 10.1002/ange.201505700es_ES
dc.identifier.e-issn1433-7851-
dc.contributor.funderMinisterio de Educación y Ciencia (España)es_ES
dc.relation.csices_ES
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