Adenosine receptors (AR) belong to the G-protein coupled receptor family. There are four receptor subtypes: A₁, A_2A, A_2B e A₃. Adenosine receptor subtypes show a different distribution in the organism and are implicated in several physiopathological processes. In particular, antagonists towards A1AR are promising in the treatment of cognitive disorders. A_2A antagonists seem to be involved in decrease the neurological impairment observed in Parkinson’s disease. A_2B antagonists are potential therapeutic agents in asthma and diabetes. Finally, antagonists at the A₃AR could be implicated in tumor growth inhibition and in glaucoma treatment. The crystallographic structure acquisition of the human A_2A receptor allowed the design of new AR antagonists by the help of computational techniques. Our group is focused on the synthesis of new adenosine receptor antagonists (particularly towards A_2A and A₃) for their potential therapeutic use, but also as tools for pharmacological investigations on these receptors.