Reverse hydroxamate-based selective TACE inhibitors

被引:30
作者
Kamei, N [1 ]
Tanaka, T [1 ]
Kawai, K [1 ]
Miyawaki, K [1 ]
Okuyama, A [1 ]
Murakami, Y [1 ]
Arakawa, Y [1 ]
Haino, M [1 ]
Harada, T [1 ]
Shimano, M [1 ]
机构
[1] Kaken Pharmaceut Co Ltd, Yamashina Ku, Kyoto 6078042, Japan
关键词
D O I
10.1016/j.bmcl.2004.03.048
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Reverse hydroxamate-based selective TACE inhibitors are described. They have potent TACE inhibitory activities and excellent selectivities against MMP-1, 2, 3, 8, 9, 13, 14, and 17. One representative compound, 18 has demonstrated an excellent oral inhibitory activity of the lipopolysaccharide (LPS)-stimulated TNF-alpha production in rats. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2897 / 2900
页数:4
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