α,β-cyclic-β-benzamido hydroxamic acids:: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE)

被引：35

作者：

Ott, Gregory R. ^{[1
]}

Asakawa, Naoyuki ^{[1
]}

Lu, Zhonghui ^{[1
]}

Liu, Rui-Qin ^{[1
]}

Covington, Maryanne B. ^{[1
]}

Vaddi, Krishna ^{[1
]}

Qian, Mingxin ^{[1
]}

Newton, Robert C. ^{[1
]}

Christ, David D. ^{[1
]}

Traskos, James M. ^{[1
]}

James, Carl P. Decicco ^{[1
]}

机构：

[1] Bristol Myers Squibb Res & Dev, Dept Discovery Chem & Discovery Biol, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 02期

关键词：

TNF-alpha; tumor necrosis factor-alpha converting enzyme; TACE; matrix metalloproteinase; MMP; beta-amino acid;

D O I：

10.1016/j.bmcl.2007.11.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Selective inhibitors of TNF-alpha Converting Enzyme (TACE) based on (1R,2S)-cyclopentyl, (3S,4S)-pyrrolidinyl, and (3R,4S)-tetrahydrofuranyl beta-benzamido hydroxamic acids have been synthesized and evaluated. This study has led to the discovery of novel inhibitors whose profiles include activity against TACE in an enzyme assay, potency in the suppression of LPS-stimulated TNF-alpha in human whole blood, selectivity against a panel of MMPs and oral bioavailability. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：694 / 699

页数：6

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