Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor

被引：40

作者：

Oh, YS ^{[1
]}

Yun, M ^{[1
]}

Hwang, SY ^{[1
]}

Hong, S ^{[1
]}

Shin, Y ^{[1
]}

Lee, K ^{[1
]}

Yoon, KH ^{[1
]}

Yoo, YJ ^{[1
]}

Kim, DS ^{[1
]}

Lee, SH ^{[1
]}

Lee, YH ^{[1
]}

Park, HD ^{[1
]}

Lee, CH ^{[1
]}

Lee, SK ^{[1
]}

Kim, S ^{[1
]}

机构：

[1] LG Chem LTD, Biotech Res Inst, Taejon 305600, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(98)00079-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Systematic variation of the so-called P-pocket moiety of benzamidrazone-based selective thrombin inhibitors led to the discovery of LB30057. It is potent (Ki = 0.38 nM for human thrombin), selective (Ki = 3290 nM for bovine trypsin), and orally bioavailable (58% oral bioavailability in dogs). LB30057 was efficacious in thrombosis animal models. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：631 / 634

页数：4

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