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
Journal of Medicinal Chemistry2007Vol. 50(11), pp. 2732–2736
Citations Over TimeTop 14% of 2007 papers
Bernat Vidal, Arsenio Nueda, Cristina Esteve, Teresa Domènech, Sonia Benito, Raquel F. Reinoso, Mercè Pont, Marta Calbet, Rosa López-Gigosos, Marı́a Isabel Cadavid, Marı́a Isabel Loza, Á. de Pablo Cárdenas, Núria Godessart, Jörge Beleta, Graham J. Warrellow, Hamish Ryder
Abstract
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 (Ki = 17 nM), good selectivity (IC(50): A(1) > 1000 nM, A(2A) > 2500 nM, A3 > 1000 nM), displayed a favorable pharmacokinetic profile in preclinical species, and showed efficacy in functional in vitro models.
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