Utilize este identificador para referenciar este registo:
https://hdl.handle.net/1822/72857
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Campo DC | Valor | Idioma |
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dc.contributor.author | Areias, Filipe | por |
dc.contributor.author | Correia, Carla | por |
dc.contributor.author | Rocha, Ashly | por |
dc.contributor.author | Brea, José | por |
dc.contributor.author | Castro, Marián | por |
dc.contributor.author | Loza, Maria I. | por |
dc.contributor.author | Proença, M. Fernanda R. P. | por |
dc.contributor.author | Carvalho, M. Alice | por |
dc.date.accessioned | 2021-05-26T10:40:48Z | - |
dc.date.issued | 2019 | - |
dc.identifier.citation | Areias, 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.2019.06.034 | por |
dc.identifier.issn | 0968-0896 | por |
dc.identifier.uri | https://hdl.handle.net/1822/72857 | - |
dc.description | Supplementary data to this article can be found online at https://doi.org/10.1016/j.bmc.2019.06.034 | por |
dc.description.abstract | From 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.sponsorship | This 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.iso | eng | por |
dc.publisher | Elsevier | por |
dc.relation | info:eu-repo/grantAgreement/FCT/3599-PPCDT/82769/PT | por |
dc.relation | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FQUI%2F00686%2F2013/PT | por |
dc.relation | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FQUI%2F0686%2F2016/PT | por |
dc.relation | info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F26106%2F2005/PT | por |
dc.relation | info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F22270%2F2005/PT | por |
dc.relation | info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F85937%2F2012/PT | por |
dc.rights | restrictedAccess | por |
dc.subject | Humans | por |
dc.subject | Molecular Structure | por |
dc.subject | Purinergic P1 Receptor Antagonists | por |
dc.subject | Structure-Activity Relationship | por |
dc.subject | Adenine derivatives | por |
dc.subject | Adenosine receptor antagonists | por |
dc.subject | 2-Arylpurine derivatives | por |
dc.title | 2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships | por |
dc.type | article | por |
dc.peerreviewed | yes | por |
dc.relation.publisherversion | https://www.sciencedirect.com/science/article/pii/S0968089619303931 | por |
oaire.citationStartPage | 3551 | por |
oaire.citationEndPage | 3558 | por |
oaire.citationIssue | 16 | por |
oaire.citationVolume | 27 | por |
dc.identifier.doi | 10.1016/j.bmc.2019.06.034 | por |
dc.date.embargo | 10000-01-01 | - |
dc.identifier.pmid | 31280999 | por |
dc.subject.fos | Ciências Naturais::Ciências Químicas | por |
dc.subject.wos | Science & Technology | por |
sdum.journal | Bioorganic & Medicinal Chemistry | por |
Aparece nas coleções: | CDQuim - Artigos (Papers) |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
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2-Aryladenine derivatives.pdf Acesso restrito! | 778,64 kB | Adobe PDF | Ver/Abrir |