N6-1,3-Diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: Synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors

Some 1-[4-(9-benzyl-2-phenyl-9H-purin-6-ylamino)-phenyl]-3-phenyl-urea derivatives and some 1-[4-(9-benzyl-2-phenyl-9H-8-azapurin-6-ylamino)-phenyl]-3-phenyl-urea derivatives were synthesised and evaluated for their interaction with adenosine receptors. It was found that some of these compounds can act as positive enhancers of agonist and antagonist radioligands for the A2A adenosine receptors. This evidence was also strengthened by functional data. Other compounds can act as negative modulators.Furthermore these compounds show inhibitory properties for A1 and A3 adenosine receptors.

Graphical abstractIt was found that some of these compounds can act as positive enhancers of agonist and antagonist radioligands for A2A adenosine receptors; other compounds can act as negative modulators.Figure optionsDownload full-size imageDownload as PowerPoint slide