ALPHA-HYDROXYESTER AND ALPHA-KETOESTER FUNCTIONALIZED THROMBIN INHIBITORS

被引：46

作者：

IWANOWICZ, EJ

LIN, J

ROBERTS, DGM

MICHEL, IM

SEILER, SM

机构：

[1] Bristol-Myers Squibb Pharmaceutical Research Institute Princeton

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(00)80440-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

alpha-Hydroxy- and alpha-ketoester functionalized D-Phe-Pro-Lys tripeptides were found to be potent thrombin active site inhibitors. The ketoester derivatives were characterized by slow binding kinetics. The most potent of the series was 9 (BMS 181,412) with an overall inhibition constant K(i)* of 0.00 17 muM.

引用

页码：1607 / 1612

页数：6

共 19 条

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