Please use this identifier to cite or link to this item: https://hdl.handle.net/1822/72857

Title2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships
Author(s)Areias, Filipe
Correia, Carla
Rocha, Ashly
Brea, José
Castro, Marián
Loza, Maria I.
Proença, M. Fernanda R. P.
Carvalho, M. Alice
KeywordsHumans
Molecular Structure
Purinergic P1 Receptor Antagonists
Structure-Activity Relationship
Adenine derivatives
Adenosine receptor antagonists
2-Arylpurine derivatives
Issue date2019
PublisherElsevier
JournalBioorganic & Medicinal Chemistry
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.2019.06.034
Abstract(s)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.
TypeArticle
DescriptionSupplementary data to this article can be found online at https://doi.org/10.1016/j.bmc.2019.06.034
URIhttps://hdl.handle.net/1822/72857
DOI10.1016/j.bmc.2019.06.034
ISSN0968-0896
Publisher versionhttps://www.sciencedirect.com/science/article/pii/S0968089619303931
Peer-Reviewedyes
AccessRestricted access (UMinho)
Appears in Collections:CDQuim - Artigos (Papers)

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