The discovery of orally available thrombin inhibitors: Optimisation of the P1 pharmacophore

被引：8

作者：

Ambler, J ^{[1
]}

Bentley, D ^{[1
]}

Brown, L ^{[1
]}

Dunnet, K ^{[1
]}

Farr, D ^{[1
]}

Janus, D ^{[1
]}

Le Grand, D ^{[1
]}

Menear, K ^{[1
]}

Mercer, M ^{[1
]}

Talbot, M ^{[1
]}

Tweed, M ^{[1
]}

Wathey, B ^{[1
]}

机构：

[1] Novartis Horsham Res Ctr, Horsham RH12 4AB, W Sussex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(99)00138-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thrombin inhibitors have been designed with the replacement of the strongly basic guanidine P1 pharmocophore with a group that exploits the lipophilicty of the S1 pocket. The approach has lead to the discovery of potent thrombin inhibitors demonstrating good intra-duodenal absorption. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1103 / 1108

页数：6

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