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 …

B Vidal, A Nueda, C Esteve, T Domenech…

文献索引：Vidal, Bernat; Nueda, Arsenio; Esteve, Cristina; Domenech, Teresa; Benito, Sonia; Reinoso, Raquel F.; Pont, Merce; Calbet, Marta; Lopez, Rosa; Cadavid, Maria Isabel; Loza, Maria Isabel; Cardenas, Alvaro; Godessart, Nuria; Beleta, Jorge; Warrellow, Graham; Ryder, Hamish Journal of Medicinal Chemistry, 2007 , vol. 50, # 11 p. 2732 - 2736

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被引用次数: 30

摘要

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 (K i= 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.