Irreversible inhibition of zinc-containing protease by oxazolidinone derivatives. Novel inactivation chemistry

被引：10

作者：

Kim, DH

Chung, SJ

Kim, EJ

Tian, GR

机构：

[1] Pohang Univ Sci & Technol, Ctr Biofunct Mol, Pohang 790784, South Korea

[2] Pohang Univ Sci & Technol, Dept Chem, Pohang 790784, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(98)00123-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

alpha-Benzyl-2-oxo-1,3-oxazolidine-4-acetic acid (BOOA) having (alpha R,4S) and (alpha S,4R) configurations were designed and synthesized as a novel type of mechanism-based inactivators for carboxypeptidase A (CPA), and kinetic analysis demonstrated that they indeed inhibit the enzyme in a time-dependent manner with the second order inhibitory rate constants (k(inact)/K-I) of 1.52 and 1.39 M-1 s(-1) for (alpha S,4R)-BOOA and (alpha R,4S)-BOOA, respectively. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：859 / 864

页数：6

共 24 条

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[2]

BINDING OF BY-PRODUCT ANALOG BENZYLSUCCINIC ACID BY CARBOXYPEPTIDASE A [J].