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- Title
2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives.
- Authors
Areias, Filipe; Correia, Carla; Rocha, Ashly; Teixeira, Sofia; Castro, Marián; Brea, Jose; Hu, Huabin; Carlsson, Jens; Loza, Maria I.; Proença, M. Fernanda; Carvalho, M. Alice
- Abstract
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.
- Subjects
ADENOSINE derivatives; ADENOSINES; RADIOLIGAND assay; STRUCTURE-activity relationships; G protein coupled receptors; PURINES
- Publication
Molecules, 2024, Vol 29, Issue 11, p2543
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules29112543