Anthranilamide inhibitors of factor Xa

被引：18

作者：

Mendel, David ^{[1
]}

Marquart, Angela L. ^{[1
]}

Joseph, Sajan ^{[1
]}

Waid, Philip ^{[1
]}

Yee, Ying K. ^{[1
]}

Tebbe, Anne Louise ^{[1
]}

Ratz, Andrew M. ^{[1
]}

Herron, David K. ^{[1
]}

Goodson, Theodore ^{[1
]}

Masters, John J. ^{[1
]}

Franciskovich, Jeffry B. ^{[1
]}

Tinsley, Jennifer M. ^{[1
]}

Wiley, Michael R. ^{[1
]}

Weir, Leonard C. ^{[1
]}

Kyle, Jeffrey A. ^{[1
]}

Klimkowski, Valentine J. ^{[1
]}

Smith, Gerald F. ^{[1
]}

Towner, Richard D. ^{[1
]}

Froelich, Larry L. ^{[1
]}

Buben, John ^{[1
]}

Craft, Trelia J. ^{[1
]}

机构：

[1] Eli Lilly & Co, Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 17期

关键词：

protease inhibitor; factor Xa; anticoagulant;

D O I：

10.1016/j.bmcl.2007.06.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

SAR about the B-ring of a series of N-2-aroyl anthranilamide factor Xa (tXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4832 / 4836

页数：5

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