2. Academic Validation
  3. 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

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

Affiliation

  • 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.

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