The design and synthesis of sulfonamides as caspase-1 inhibitors

被引：56

作者：

Harter, WG

Albrect, H

Brady, K

Caprathe, B

Dunbar, J

Gilmore, J

Hays, S

Kostlan, CR

Lunney, B

Walker, N

机构：

[1] Pfizer Global Res & Dev, Dept Chem, Ann Arbor, MI 48105 USA

[2] Abbott, Ludwigshafen, Germany

[3] Abbott, Worcester, MA USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

D O I：

10.1016/j.bmcl.2003.10.065

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of sulfonamides (1) has been prepared as inhibitors of interleukin-1beta converting enzyme (ICE), also known as caspase 1. These compounds were designed to improve potency by rigidifying the enzyme bound molecule through an intramolecular hydrogen bond. An X-ray crystal structure of a representative member of this series bound to the active site of ICE, confirms the presence of the hydrogen bonding interaction. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：809 / 812

页数：4

共 38 条

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