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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6845-9. doi: 10.1016/j.bmcl.2010.08.064. Epub 2010 Aug 19.

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

Author information

1
Ligand Pharmaceuticals, Inc., 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA. bmcguinness@venenumbiodesign.com

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.

PMID:
20869242
DOI:
10.1016/j.bmcl.2010.08.064
[Indexed for MEDLINE]

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