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

  • J Med Chem. 2007 May 31;50(11):2732-6. doi: 10.1021/jm061333v.
Bernat Vidal  1 ,  Arsenio Nueda ,  Cristina Esteve ,  Teresa Domenech ,  Sonia Benito ,  Raquel F Reinoso ,  Mercè Pont ,  Marta Calbet ,  Rosa López ,  María Isabel Cadavid ,  María Isabel Loza ,  Alvaro Cárdenas ,  Núria Godessart ,  Jorge Beleta ,  Graham Warrellow ,  Hamish Ryder
Affiliations
  • 1. Almirall Research Center, Almirall, Ctra. Laureà Miró 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain. [email protected]
PMID: 17469811 DOI: 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 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.

Products