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

P Eastwood, J Gonzalez, S Paredes, A Nueda…

Index: Eastwood, Paul; Gonzalez, Jacob; Paredes, Sergio; Nueda, Arsenio; Domenech, Teresa; Alberti, Joan; Vidal, Bernat Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 5 p. 1697 - 1700

Full Text: HTML

Citation Number: 12

Abstract

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.