Discovery and Characterization of 4‘-(2-Furyl)-N-pyridin-3-yl-4,5‘-bipyrimidin-2‘-amine (LAS38096), a Potent, Selective, and Efficacious A2BAdenosine Receptor Antagonist
- 1 May 2007
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 50 (11) , 2732-2736
- https://doi.org/10.1021/jm061333v
Abstract
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.Keywords
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