2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives.

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Areias F, Correia C, Rocha A, Teixeira S, Castro M, Brea J, Hu H, Carlsson J, Loza MI, Proença MF, Carvalho MA

Molecules 29 (11) - [2024-05-28; online 2024-05-28]

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.

PubMed 38893418

DOI 10.3390/molecules29112543

Crossref 10.3390/molecules29112543

pmc: PMC11173536
pii: molecules29112543