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

被引：33

作者：

Becker, DP

DeCrescenzo, G

Freskos, J

Getman, DP

Hockerman, SL

Li, M

Mehta, P

Munie, GE

Swearingen, C

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)00557-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of alpha -alkyl-alpha -amino-beta -sulphone hydroxamates was prepared and evaluated for potency versus MMP-2 and NIMP-13, and for selectivity versus MMP-1. Low nanomolar potency was obtained with selectivity versus MMP-1 ranging from >10 to >1000. Selected compounds were orally bioavailable. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：2723 / 2725

页数：3

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