Discovery of novel FMS kinase inhibitors as anti-inflammatory agents

被引:44
|
作者
Illig, Carl R. [1 ]
Chen, Jinsheng [1 ]
Wall, Mark J. [1 ]
Wilson, Kenneth J. [1 ]
Ballentine, Shelley K. [1 ]
Rudolph, M. Jonathan [1 ]
DesJarlais, Renee L. [1 ]
Chen, Yanmin [1 ]
Schubert, Carsten [1 ]
Petrounia, Ioanna [1 ]
Crysler, Carl S. [1 ]
Molloy, Christopher J. [1 ]
Chaikin, Margery A. [1 ]
Manthey, Carl L. [1 ]
Player, Mark R. [1 ]
Tomczuk, Bruce E. [1 ]
Meegalla, Sanath K. [1 ]
机构
[1] Johnson & Johnson Pharmaceut Res & Dev, Spring House, PA 19477 USA
关键词
FMS; CSF-1R; M-CSF; colony stimulating factor-1; macrophages; anti-inflammatory activity;
D O I
10.1016/j.bmcl.2008.01.059
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The optimization of the arylamide lead 2 resulted in identification of a highly potent series of 2,4-disubstituted arylamides. Compound 8 (FMS kinase IC50 = 0.0008 mu M) served as a proof-of-concept candidate in a collagen-induced model of arthritis in mice. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1642 / 1648
页数:7
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