The discovery of orally available thrombin inhibitors: Studies towards the optimisation of CGH1668

被引：12

作者：

Ambler, J ^{[1
]}

Baker, E ^{[1
]}

Brown, L ^{[1
]}

Butler, P ^{[1
]}

Farr, D ^{[1
]}

Dunnet, K ^{[1
]}

Le Grand, D ^{[1
]}

Janus, D ^{[1
]}

Jones, D ^{[1
]}

Menear, K ^{[1
]}

Mercer, M ^{[1
]}

Smith, G ^{[1
]}

Talbot, M ^{[1
]}

Tweed, M ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(98)00640-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The chemical optimisation of CGH1668 1 is described employing an in vivo model of absorption to determine the influence on bioavailability of single Feint modifications to five key molecular templates. The discovery of an orally bioavailable and selective thrombin inhibitor, 24, highlights the utility of this approach. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3583 / 3588

页数：6

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