Author(s):
Areias, Filipe ; Correia, Carla ; Rocha, Ashly ; Teixeira, Sofia ; Castro, Marián ; Brea, Jose ; Hu, Huabin ; Carlsson, Jens ; Loza, Maria I. ; Proença, M. Fernanda R. P. ; Carvalho, M. Alice
Date: 2024
Persistent ID: https://hdl.handle.net/1822/97751
Origin: RepositóriUM - Universidade do Minho
Subject(s): 2-arylpurine derivatives; adenine derivatives; adenosine receptor antagonists; G protein-coupled receptors; structure-activity relationship
Description
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.
