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α-amino-β-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1

被引：40
作者：
Becker, DP
Barta, TE
Bedell, L
DeCrescenzo, G
Freskos, J
Getman, DP
Hockerman, SL
Li, M
Mehta, P
Mischke, B
Munie, GE
Swearingen, C
Villamil, CL
机构：
[1] Pharmacia Res & Dev, Dept Med Chem, Skokie, IL 60077 USA
[2] Pharmacia Res & Dev, Dept Inflammat Oncol, Skokie, IL 60077 USA
[3] Pharmacia Res & Dev, Dept Med Chem, St Louis, MO 63198 USA
[4] Pharmacia Res & Dev, Dept Inflammat Oncol, St Louis, MO 63198 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(01)00556-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of alpha -amino-beta -sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and selectivity versus MMP-1. Various substituents were employed on the alpha -amino group (P-1 position), as well as different groups attached to the sulphone group extending into P-1'. Low nanomolar potency was obtained for MMP-13 with selectivity versus MMP-1 of > 1000x for a number of analogues. (C) 2001 Elsevier Science Ltd. All rights reserved.
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收藏
页码：2719 / 2722
页数：4
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