新型喹啉酮腺苷 A2B 拮抗剂的发现。
Discovery of novel quinolinone adenosine A2B antagonists.
机构信息
Ligand Pharmaceuticals, 3000 Eastpark Boulevard Cranbury, NJ 08512, USA.
出版信息
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7414-20. doi: 10.1016/j.bmcl.2010.10.030. Epub 2010 Nov 4.
PMID:21055932
Abstract
A novel series of quinolinone-based adenosine A(2B) receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features of the initial hit. Optimization resulted in an A(2B) antagonist (2i) which exhibited potent activity in a cAMP accumulation assay (5.1 nM) and an IL-8 release assay (0.4 nM).
摘要
通过高通量筛选编码组合化合物库，发现了一系列新型喹啉酮类腺嘌呤 A(2B)受体拮抗剂。对一系列类似物的合成和测定突出了初始命中物的基本结构特征。优化得到的 A(2B)拮抗剂（2i）在 cAMP 积累测定（5.1 nM）和 IL-8 释放测定（0.4 nM）中表现出很强的活性。
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