Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A2B adenosine receptor antagonists

The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A2B adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat.

Graphical abstractThe potent and selective A2B adenosine receptor antagonist 9 was shown to have good oral bioavailability in the rat.Figure optionsDownload full-size imageDownload as PowerPoint slide