Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists.
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.
McGuinness
Brian F
BF
Ligand Pharmaceuticals, Inc., 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA. bmcguinness@venenumbiodesign.com
Cole
Andrew G
AG
Dong
Guizhen
G
Brescia
Marc-Raleigh
MR
Shao
Yuefei
Y
Henderson
Ian
I
Rokosz
Laura L
LL
Stauffer
Tara M
TM
Mannava
Neelima
N
Kimble
Earl F
EF
Hicks
Catherine
C
White
Nicole
N
Wines
Pamela G
PG
Quadros
Elizabeth
E
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*
D011743:Pyrimidines; D043705:Receptor, Adenosine A2A