Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors

被引：15

作者：

Dener, JM

Wang, VR

Rice, KD

Gangloff, AR

Kuo, EYL

Newcomb, WS

Putnam, D

Wong, M

机构：

[1] Axys Pharmaceut Inc, Dept Med Chem, S San Francisco, CA 94080 USA

[2] Axys Pharmaceut Inc, Dept Biochem, S San Francisco, CA 94080 USA

[3] Axys Pharmaceut Inc, Dept Enzymol, S San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(01)00444-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Truncation of potent and selective dibasic inhibitors afforded monocharged inhibitors of human mast-cell tryptase. Using two classes of analogues as lead structures, several monocharged derivatives were identified with Ki values ranging front 0.084 to 0.21 muM against the enzyme. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：2325 / 2330

页数：6

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