2-Aryladenine derivatives as a potent scaffold for adenosine receptor antagonists: The 6-Morpholino derivatives

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dc.contributor.authorAreias, Filipe
dc.contributor.authorCorreia, Carla
dc.contributor.authorRocha, Ashly
dc.contributor.authorTeixeira, Sofia
dc.contributor.authorCastro, Marián
dc.contributor.authorBrea, Jose
dc.contributor.authorHu, Huabin
dc.contributor.authorCarlsson, Jens
dc.contributor.authorLoza, Maria I.
dc.contributor.authorProença, M. Fernanda R. P.
dc.contributor.authorCarvalho, M. Alice
dc.date.accessioned2025-10-23T14:42:28Z
dc.date.issued2024-06-01
dc.date.updated2025-10-23T09:56:00Z
dc.description.abstractA set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A<inf>1</inf>, A<inf>2A</inf>, A<inf>2B</inf>, and A<inf>3</inf> adenosine receptor subtypes. Eleven purines showed potent antagonism at A<inf>1</inf>, A<inf>3</inf>, dual A<inf>1</inf>/A<inf>2A</inf>, A<inf>1</inf>/A<inf>2B</inf>, or A<inf>1</inf>/A<inf>3</inf> adenosine receptors. Additionally, three compounds showed high affinity without selectivity for any specific adenosine receptor. The structure-activity relationships were made for this group of new compounds. The 9-methylpurine derivatives were generally less potent but more selective, and the 9H-purine derivatives were more potent but less selective. These compounds can be an important source of new biochemical tools and/or pharmacological drugs.eng
dc.description.sponsorshipThis research was funded by the Portuguese Fundação para a Ciência e Tecnologia/Ministério da Educação e Ciência (MEC) through funds in the framework of the Strategic Funding of CQUM (UID/QUI/00686/2020), (UID/QUI/00686/2018), FEDER funds through the Operational Programme for Competitiveness Factors (COMPETE 2020), Programa Operacional de Competitividade e Internacionalização (POCI) (POCI-01-0145-FEDER-031354) Rede Nacional de RMN (PINFRA/22161/2016), and PhD grants to Carla Correia and Ashly Rocha (SFRH/BD/22270/2005; SFRH/BD/85937/2012), Xunta de Galicia (ED431C 2022/20), and the European Regional Development Fund (ERDF). Filipe Areias gratefully acknowledges the Post-PhD grant from the Portuguese FCT (SFRH/BPD/26106/2005). J.C. received funding from the Olle Engkvist Foundation (219-0154) and the Swedish Research Council (2021-4186). The LECO instrument for elemental analysis TruSpec Micro CHN was purchased within the PT-OPENSCREEN project (NORTE-01—0145-FEDER-085468), financed by CCDR-N.
dc.distributioninternational
dc.identifier.citationAreias, F., Correia, C., Rocha, A., Teixeira, S., Castro, M., Brea, J., Hu, H., Carlsson, J., Loza, M. I., Proença, M. F., & Carvalho, M. A. (2024). 2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives. Molecules, 29(11), 2543. https://doi.org/10.3390/molecules29112543
dc.identifier.doi10.3390/molecules29112543
dc.identifier.eissn1420-3049
dc.identifier.pmc38893418
dc.identifier.pmid38893418por
dc.identifier.urihttps://hdl.handle.net/1822/97751
dc.language.isoeng
dc.peerreviewedyes
dc.publisherMultidisciplinary Digital Publishing Institute (MDPI)
dc.relationChemistry Center - University of Minho [UIDP/00686/2020]
dc.relationChemistry Center - University of Minho [UIDB/00686/2020]
dc.relationPortuguese Nuclear Magnetic Resonance Network [PINFRA/22161/2016]
dc.relationSíntese de novos heterociclos com potencial actividade anticancerígena baseada em estudos de virtual screening farmacológico [SFRH/BD/85937/2012]
dc.relationEsquizofrenia: Screening farmacológico [SFRH/BPD/26106/2005]
dc.relationSíntese e determinação da potencial acção antioxidante de oxopirroles e derivados/análogos de purina [SFRH/BD/22270/2005]
dc.relationUIDP/QUI/00686/2018
dc.relation.hasversionhttps://www.mdpi.com/1420-3049/29/11/2543
dc.rightsopenAccess
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subject2-arylpurine derivatives
dc.subjectadenine derivatives
dc.subjectadenosine receptor antagonists
dc.subjectG protein-coupled receptors
dc.subjectstructure-activity relationship
dc.subject.fosCiências Naturais::Ciências Químicas
dc.title2-Aryladenine derivatives as a potent scaffold for adenosine receptor antagonists: The 6-Morpholino derivativeseng
dc.typearticle
dspace.entity.typePublication
oaire.awardNumberUIDP/00686/2020
oaire.awardNumberUIDB/00686/2020
oaire.awardNumberPINFRA/22161/2016
oaire.awardNumberSFRH/BD/85937/2012
oaire.awardNumberSFRH/BPD/26106/2005
oaire.awardNumberSFRH/BD/22270/2005
oaire.awardTitleChemistry Center - University of Minho [UIDP/00686/2020]
oaire.awardTitleChemistry Center - University of Minho [UIDB/00686/2020]
oaire.awardTitlePortuguese Nuclear Magnetic Resonance Network [PINFRA/22161/2016]
oaire.awardTitleSíntese de novos heterociclos com potencial actividade anticancerígena baseada em estudos de virtual screening farmacológico [SFRH/BD/85937/2012]
oaire.awardTitleEsquizofrenia: Screening farmacológico [SFRH/BPD/26106/2005]
oaire.awardTitleSíntese e determinação da potencial acção antioxidante de oxopirroles e derivados/análogos de purina [SFRH/BD/22270/2005]
oaire.awardURIhttps://hdl.handle.net/1822/97652
oaire.awardURIhttps://hdl.handle.net/1822/97651
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oaire.awardURIhttps://hdl.handle.net/1822/97746
oaire.citationIssue11
oaire.citationVolume29
oaire.funderIdentifierhttp://doi.org/10.13039/501100001871
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oaire.funderIdentifierhttp://doi.org/10.13039/501100001871
oaire.funderNameFundação para a Ciência e a Tecnologia, I.P.
oaire.funderNameFundação para a Ciência e a Tecnologia, I.P.
oaire.funderNameFundação para a Ciência e a Tecnologia, I.P.
oaire.funderNameFundação para a Ciência e a Tecnologia, I.P.
oaire.funderNameFundação para a Ciência e a Tecnologia, I.P.
oaire.funderNameFundação para a Ciência e a Tecnologia, I.P.
oaire.fundingStreamConcurso de avaliação no âmbito do Programa Plurianual de Financiamento de Unidades de I&D (2017/2018) - Financiamento Programático
oaire.fundingStreamConcurso de avaliação no âmbito do Programa Plurianual de Financiamento de Unidades de I&D (2017/2018) - Financiamento Base
oaire.fundingStreamConcurso para Financiamento de Projetos de Infraestruturas de Investigação inseridas no Roteiro Nacional de Infraestruturas de Investigação de Interesse Estratégico
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sdum.export.identifier18736
sdum.journalMolecules

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