Utilize este identificador para referenciar este registo: https://hdl.handle.net/1822/72857

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dc.contributor.authorAreias, Filipepor
dc.contributor.authorCorreia, Carlapor
dc.contributor.authorRocha, Ashlypor
dc.contributor.authorBrea, Josépor
dc.contributor.authorCastro, Mariánpor
dc.contributor.authorLoza, Maria I.por
dc.contributor.authorProença, M. Fernanda R. P.por
dc.contributor.authorCarvalho, M. Alicepor
dc.date.accessioned2021-05-26T10:40:48Z-
dc.date.issued2019-
dc.identifier.citationAreias, F., Correia, C., Rocha, A., Brea, J., Castro, M., Loza, M. I., . . . Carvalho, M. A. (2019). 2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships. Bioorganic & Medicinal Chemistry, 27(16), 3551-3558. doi: https://doi.org/10.1016/j.bmc.2019.06.034por
dc.identifier.issn0968-0896por
dc.identifier.urihttps://hdl.handle.net/1822/72857-
dc.descriptionSupplementary data to this article can be found online at https://doi.org/10.1016/j.bmc.2019.06.034por
dc.description.abstractFrom a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A1 adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of 24 purines was synthesized and tested in radioligand binding assays at human A1, A2A, A2B and A3 adenosine receptor subtypes. Fourteen molecules showed potent antagonism at A1, A3 or dual A1/A3 adenosine receptors. This purine scaffold is an important source for novel biochemical tools and/or therapeutic drugs.por
dc.description.sponsorshipThis research was funded by the Spanish Ministry of Science and Innovation, Spain (grants HF2007-0055 and BIO2008-02329), the Portuguese Fundação para a Ciência e Tecnologia (PPCDT/QUI/59356/2004), the Xunta de Galicia, Spain (07CSA003203PR and 08CSA020203PR), and the Carlos III Health Institute, Spain. Funds provided by FCT through the Chemistry Research Centre of the University of Minho (Ref. UID/QUI/00686/2013 and UID/QUI/0686/2016) are also gratefully acknowledged. Filipe Areias gratefully ac knowledge Post-PhD grants from the Portuguese FCT (SFRH/BPD/26106/2005). Carla Correia and Ashly Rocha also acknowledge to FCT the PhD grants (SFRH/BD/22270/2005; SFRH/BD/85937/2012). The NMR spectrometer (Bruker 400 Avance III) is part of the National NMR Network supported by funds from FCT.por
dc.language.isoengpor
dc.publisherElsevierpor
dc.relationinfo:eu-repo/grantAgreement/FCT/3599-PPCDT/82769/PTpor
dc.relationinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FQUI%2F00686%2F2013/PTpor
dc.relationinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FQUI%2F0686%2F2016/PTpor
dc.relationinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F26106%2F2005/PTpor
dc.relationinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F22270%2F2005/PTpor
dc.relationinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F85937%2F2012/PTpor
dc.rightsrestrictedAccesspor
dc.subjectHumanspor
dc.subjectMolecular Structurepor
dc.subjectPurinergic P1 Receptor Antagonistspor
dc.subjectStructure-Activity Relationshippor
dc.subjectAdenine derivativespor
dc.subjectAdenosine receptor antagonistspor
dc.subject2-Arylpurine derivativespor
dc.title2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationshipspor
dc.typearticlepor
dc.peerreviewedyespor
dc.relation.publisherversionhttps://www.sciencedirect.com/science/article/pii/S0968089619303931por
oaire.citationStartPage3551por
oaire.citationEndPage3558por
oaire.citationIssue16por
oaire.citationVolume27por
dc.identifier.doi10.1016/j.bmc.2019.06.034por
dc.date.embargo10000-01-01-
dc.identifier.pmid31280999por
dc.subject.fosCiências Naturais::Ciências Químicaspor
dc.subject.wosScience & Technologypor
sdum.journalBioorganic & Medicinal Chemistrypor
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