Biaryl substituted alkylboronate esters as thrombin inhibitors

被引：12

作者：

Quan, ML

Wityak, J

Dominguez, C

Duncia, JV

Kettner, CA

Ellis, CD

Liauw, AY

Park, JM

Santella, JB

Knabb, RM

Thoolen, MJ

Weber, PC

Wexler, RR

机构：

[1] DuPont Merck Pharmaceutical Company, P.O. Box 80500, Wilmington

[2] Schering Plough Research, Kenilworth

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(97)00254-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thrombin is a serine protease that plays an important role in the blood coagulation cascade, and is a target enzyme for new therapeutic agents. Ac-(D)-Phe-Pro-boroArg-OH (DuP714) was found to be a highly effective thrombin inhibitor. In order to reduce the peptidic nature of DuP 714, we have designed a series of novel biaryl substituted alkylboronate esters as potent thrombin inhibitors. The most potent compounds have subnanomolar affinity for thrombin. (C) 1997 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd.

引用

页码：1595 / 1600

页数：6

共 10 条

[1] AROMATIC-AROMATIC INTERACTION - A MECHANISM OF PROTEIN-STRUCTURE STABILIZATION [J].