Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.

A novel series of N-heteroaryl 4‘-(2-furyl)-4,5‘-bipyrimidin-2‘-amines has been identified as potent and selective A2B adenosine receptor antagonists. In particular, compound 5 showed high affinity for the A2B receptor (Ki = 17 nM), good selectivity (IC50:  A1 > 1000 nM, A2A > 2500 nM, A3 > 1000 nM), displayed a favorable pharmacokinetic profile in preclinical species, and showed efficacy in functional in vitro models.