Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors

被引：23

作者：

Palmer, JT ^{[1
]}

Rydzewski, RM ^{[1
]}

Mendonca, RV ^{[1
]}

Sperandio, D ^{[1
]}

Spencer, JR ^{[1
]}

Hirschbein, BL ^{[1
]}

Lohman, J ^{[1
]}

Beltman, J ^{[1
]}

Nguyen, M ^{[1
]}

Liu, L ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 13期

关键词：

tryptase; serine protease; inhibitor; heterocycle; ketoheterocycle; selective; scaleable process; pharmacokinetics;

D O I：

10.1016/j.bmcl.2006.04.013

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using a scaleable, directed library approach based on orthogonally protected advanced intermediates, we have prepared a series of potent keto-1,2,4-oxadiazoles designed to explore the P-2 binding pocket of human mast cell tryptase, while building in a high degree of selectivity over human trypsin and other serine proteases. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3434 / 3439

页数：6

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