title: Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists.
abstract: A novel series of adenosine A(2A) receptor antagonists was identified by high-throughput screening of an encoded combinatorial compound collection. The initial hits were optimized for A(2A) binding affinity, A(1) selectivity, and in vitro microsomal stability generating orally available 2-aminoimidazo[4,5-b]pyridine-based A(2A) antagonist leads.
authors.affiliation: Ligand Pharmaceuticals, Inc., 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA. bmcguinness@venenumbiodesign.com
authors.forename: Brian F
authors.initials: BF
authors.lastname: McGuinness
authors.forename: Andrew G
authors.initials: AG
authors.lastname: Cole
authors.forename: Guizhen
authors.initials: G
authors.lastname: Dong
authors.forename: Marc-Raleigh
authors.initials: MR
authors.lastname: Brescia
authors.forename: Yuefei
authors.initials: Y
authors.lastname: Shao
authors.forename: Ian
authors.initials: I
authors.lastname: Henderson
authors.forename: Laura L
authors.initials: LL
authors.lastname: Rokosz
authors.forename: Tara M
authors.initials: TM
authors.lastname: Stauffer
authors.forename: Neelima
authors.initials: N
authors.lastname: Mannava
authors.forename: Earl F
authors.initials: EF
authors.lastname: Kimble
authors.forename: Catherine
authors.initials: C
authors.lastname: Hicks
authors.forename: Nicole
authors.initials: N
authors.lastname: White
authors.forename: Pamela G
authors.initials: PG
authors.lastname: Wines
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Quadros
mesh_terms: D055808:Drug Discovery; D006801:Humans; D006860:Hydrogen Bonding; D008861:Microsomes / Q000187:drug effects; D011743:Pyrimidines / Q000494:pharmacology*; D043705:Receptor, Adenosine A2A / Q000737:chemistry / Q000187:drug effects*
chemical_list: D011743:Pyrimidines; D043705:Receptor, Adenosine A2A