Dibasic inhibitors of human mast cell tryptase. Part 1: Synthesis and optimization of a novel class of inhibitors

被引：28

作者：

Rice, KD

Gangloff, AR

Kuo, EYL

Dener, JM

Wang, VR

Lum, R

Newcomb, WS

Havel, C

Putnam, D

Cregar, L

Wong, M

Warne, RL

机构：

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

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

[3] Exelixis Pharmaceut Inc, San Francisco, CA 94080 USA

[4] ChemRx Adv Technol, San Francisco, CA 94080 USA

[5] CV Therapeut Inc, Palo Alto, CA 94304 USA

[6] Argonaut Technol Inc, San Carlos, CA 94070 USA

[7] Chiron Corp, Emeryville, CA 94608 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(00)00484-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and optimization of a novel class of reversible and active-site directed dibasic inhibitors of human mast cell tryptase are described. The compounds were shown to be both remarkably potent and selective for tryptase with Ki values for optimized inhibitors in the picomolar range. (C) 2000 Published by Elsevier Science Ltd.

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收藏

页码：2357 / 2360

页数：4

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