5-lipoxygenase inhibitors with histamine H1 receptor antagonist activity

被引：33

作者：

Lewis, TA ^{[1
]}

Bayless, L ^{[1
]}

Eckman, JB ^{[1
]}

Ellis, JL ^{[1
]}

Grewal, G ^{[1
]}

Libertine, L ^{[1
]}

Nicolas, JM ^{[1
]}

Scannell, RT ^{[1
]}

Wels, BF ^{[1
]}

Wenberg, K ^{[1
]}

Wypij, DM ^{[1
]}

机构：

[1] UCB Res, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 09期

关键词：

D O I：

10.1016/j.bmcl.2004.02.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel compounds with both 5-lipoxygenase (5-LO) inhibitory and histamine H-1 receptor antagonist activity were designed for the treatment of asthma. These dual-function compounds were made by connecting 5-LO and H-1 pharmacophores, N-hydroxyureas and benzhydryl piperazines, respectively. A range of in vitro activities was observed, with the furan analog 10 demonstrating both activities in an animal model. The activities observed were compared to single-function drugs. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2265 / 2268

页数：4

共 21 条

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