Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors

被引：13

作者：

Lombart, Henry-Georges

Feyfant, Eric

Joseph-McCarthy, Diane

Huang, Adrian

Lovering, Frank

Sun, LinHong

Zhu, Yi

Zeng, Congmei

Zhang, Yuhua

Levin, Jeremy

机构：

[1] Wyeth Res, Chem & Screening Sci, Cambridge, MA 02140 USA

[2] Wyeth Res, Chem & Screening Sci, Pearl River, NY 10965 USA

[3] Wyeth Res, Inflammat, Cambridge, MA 02140 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 15期

关键词：

inflammation; TACE; rheumatoid arthritis;

D O I：

10.1016/j.bmcl.2007.05.022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-based methods were used to design P-sulfone 3,3-piperidine hydroxamates as TACE inhibitors with the aim of improving selectivity for TACE versus MMP-13. Several compounds in this series were synthesized and evaluated in enzymatic and cell-based assays. These analogs exhibit excellent in vitro potency against isolated TACE enzyme and show good selectivity for TACE over the related metalloproteases MMP-2, -13, and -14. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4333 / 4337

页数：5

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