Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 11, Pages 2732-2736Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm061333v
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A novel series of N-heteroaryl 4'-(2-furyl)-4,5'-bipyrimidin-2'-amines has been identified as potent and selective A(2B) adenosine receptor antagonists. In particular, compound 5 showed high affinity for the A(2B) receptor (K-i = 17 nM), good selectivity (IC50: A(1) > 1000 nM, A(2A) > 2500 nM, A(3) > 1000 nM), displayed a favorable pharmacokinetic profile in preclinical species, and showed efficacy in functional in vitro models.
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