1-aminoisoquinollne as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors

被引：53

作者：

Rewinkel, JBM ^{[1
]}

Lucas, H ^{[1
]}

van Galen, PJM ^{[1
]}

Noach, ABJ ^{[1
]}

van Dinther, TG ^{[1
]}

Rood, AMM ^{[1
]}

Jenneboer, AJSM ^{[1
]}

van Boeckel, CAA ^{[1
]}

机构：

[1] NV Organon, Sci Dev Grp, NL-5340 BH Oss, Netherlands

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(99)00069-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：685 / 690

页数：6

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