Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors

被引：24

作者：

Coburn, CA ^{[1
]}

Rush, DM

Williams, PD

Homnick, C

Lyle, EA

Lewis, SD

Lucas, BJ

Di Muzio-Mower, JM

Juliano, M

Krueger, JA

Vastag, K

Chen, IW

Vacca, JP

机构：

[1] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA

[2] Merck Res Labs, Dept Pharmacol, W Point, PA 19486 USA

[3] Merck Res Labs, Dept Biol Chem, W Point, PA 19486 USA

[4] Merck Res Labs, Dept Drug Metab, W Point, PA 19486 USA

来源：

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

关键词：

D O I：

10.1016/S0960-894X(00)00170-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new class of conformationally constrained thrombin inhibitors is described. These compounds contain a unique bicyclic pyridone scaffold which serves as a P3P2 dipeptide surrogate. The synthesis and antithrombotic activity of these inhibitors is reported. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1069 / 1072

页数：4

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