New substituted 9-propyladenine derivatives as A2Aadenosine receptor antagonists

A new series of 9-propyladenines bearing a phenylalkylamino group in the 2-position or a phenylalkyl chain in the N6-position, and further substituted with a bromine atom or a 2-furyl ring in the 8-position, were synthesized and tested at human adenosine receptors. The novel compounds proved to be A2A adenosine receptor antagonists and some of them showed high A2A affinity, but moderate selectivity (18: KiA2A = 6.6 nM). Molecular modeling studies gave some explanation of the different activities of the compounds, giving suggestions for the synthesis of new A2A adenosine receptor antagonists.