Novel, acidic CCR2 receptor antagonists: From hit to lead

被引：15
|
作者：
Zou, D.
Zhai, H. A.
Eckman, J.
Higgins, P.
Gillard, M.
Knerr, L.
Carre, S.
Pasau, P.
Collart, P.
Grassi, J.
Libertine, L.
Nicolas, J. -M.
Schwartz, C. E.
机构：
[1] UCB Res Inc, Cambridge, MA 02139 USA
[2] UCB Pharma, B-1420 Braine lAlleud, Belgium
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2007年 / 4卷 / 03期
关键词：
MCP-1; CCR2; chemokine receptor; antagonist; inflammation; hit to lead;
D O I：
10.2174/157018007780077381
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
High throughput screening identified a pyrrolidinone containing acidic functionality as a CCR2 antagonist of modest affinity. We describe initial SAR around this hit, including solution phase parallel synthesis for analog preparation, and we describe identification and characterization of an analog subsequently selected as a viable lead molecule for further optimization.
引用
收藏
页码：185 / 191
页数：7
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