Benzylamine-based selective and orally bioavailable inhibitors of thrombin

被引：29

作者：

Lee, K ^{[1
]}

Jung, WH ^{[1
]}

Park, CW ^{[1
]}

Hong, CY ^{[1
]}

Kim, IC ^{[1
]}

Kim, S ^{[1
]}

Oh, YS ^{[1
]}

Kwon, OH ^{[1
]}

Lee, SH ^{[1
]}

Park, HD ^{[1
]}

Kim, SW ^{[1
]}

Lee, YH ^{[1
]}

Yoo, YJ ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(98)00456-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of p-aminomethylphenylalanine derivatives were investigated as novel thrombin inhibitors. This study led to potent inhibitors of thrombin (Ki up to 3.3 nM) that are trypsin-selective, highly orally bioavailable in rats, and highly permeable across Caco-2 cells. The P1 benzylamine binding mode in the thrombin active site was identified by X-ray crystallographic analysis. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2563 / 2568

页数：6

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