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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.
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页码：809 / 812
页数：4
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