RT Journal Article
T1 2-Aryladenine derivatives as a potent scaffold for adenosine receptor antagonists: the 6-Morpholino derivatives
A1 Areias, Filipe
A1 Correia, Carla
A1 Rocha, Ashly
A1 Teixeira, Sofia
A1 Castro Pérez, Marián
A1 Brea Floriani, José Manuel
A1 Hu, Huabin
A1 Carlsson, Jens
A1 Loza García, María Isabel
A1 Proença, M. Fernanda
A1 Carvalho, M. Alice
K1 G protein-coupled receptors
K1 Adenine derivatives
K1 Adenosine receptor antagonists
K1 2-arylpurine derivatives
K1 Structure-activity relationship
AB A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A1, A2A, A2B, and A3 adenosine receptor subtypes. Eleven purines showed potent antagonism at A1, A3, dual A1/A2A, A1/A2B, or A1/A3 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
PB MDPI
YR 2024
FD 2024-05-28
LK https://hdl.handle.net/10347/45595
UL https://hdl.handle.net/10347/45595
LA eng
NO Areias, 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
NO This 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
DS Minerva
RD 23 abr 2026