Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists

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-aminoimida...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-11, Vol.20 (22), p.6845-6849
Hauptverfasser: McGuinness, Brian F, Cole, Andrew G, Dong, Guizhen, Brescia, Marc-Raleigh, Shao, Yuefei, Henderson, Ian, Rokosz, Laura L, Stauffer, Tara M, Mannava, Neelima, Kimble, Earl F, Hicks, Catherine, White, Nicole, Wines, Pamela G, Quadros, Elizabeth
Format: Artikel
Sprache:eng
Schlagworte:
Drug Discovery
Humans
Hydrogen Bonding
Microsomes - drug effects
Pyrimidines - pharmacology
Receptor, Adenosine A2A - chemistry
Receptor, Adenosine A2A - drug effects
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Zusammenfassung: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.
ISSN:1464-3405
DOI:10.1016/j.bmcl.2010.08.064