发现 2-氨基咪唑并吡啶腺苷 A(2A)受体拮抗剂。
Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists.
机构信息
Ligand Pharmaceuticals, Inc., 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
出版信息
Bioorg Med Chem Lett. 2010 Nov 15;20(22):6845-9. doi: 10.1016/j.bmcl.2010.08.064. Epub 2010 Aug 19.
PMID:20869242
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.
摘要
通过高通量筛选编码组合化合物文库，发现了一系列新型的腺苷 A(2A)受体拮抗剂。最初的命中化合物经过优化，提高了对 A(2A)的结合亲和力、对 A(1)的选择性以及体外微粒体稳定性，得到了可口服的 2-氨基咪唑并[4,5-b]吡啶基 A(2A)拮抗剂先导化合物。
Zotero 插件