Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption

被引：12

作者：

Lee, K ^{[1
]}

Jung, WH ^{[1
]}

Hwang, SY ^{[1
]}

Lee, SH ^{[1
]}

机构：

[1] LG Chem Ltd, Biotech Res Inst, Taejon 305380, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(99)00412-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

LB30057 (1) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound 1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity. Compound 2 demonstrated a 3-fold increase in absorption. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2483 / 2486

页数：4

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