Novel, potent, selective, and orally bioavailable human βII-tryptase inhibitors

被引：11

作者：

Sperandio, David ^{[1
]}

Tai, Vincent W. -F. ^{[1
]}

Lohman, Julia ^{[1
]}

Hirschbein, Bernie ^{[1
]}

Mendonca, Rohan ^{[1
]}

Lee, Chang-Sun ^{[1
]}

Spencer, Jeffrey R. ^{[1
]}

Janc, James ^{[1
]}

Nguyen, Margaret ^{[1
]}

Beltman, Jerlyn ^{[1
]}

Sprengeler, Paul ^{[1
]}

Scheerens, Heleen ^{[1
]}

Lin, Tong ^{[1
]}

Liu, Liang ^{[1
]}

Gadre, Ashwini ^{[1
]}

Kellogg, Alisha ^{[1
]}

Green, Michael J. ^{[1
]}

McGrath, Mary E. ^{[1
]}

机构：

[1] Celera Gen, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 15期

关键词：

D O I：

10.1016/j.bmcl.2006.04.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of novel [1,2,4]oxadiazoles and their structure-activity relationship (SAR) for the inhibition of tryptase and related serine proteases is presented. Elaboration of the P'-side afforded potent, selective, and orally bioavailable tryptase inhibitors. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4085 / 4089

页数：5

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