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Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.

Abstract：

:The coagulation factor Xa (FXa) plays a central role in the blood coagulation cascade. Recent studies have shown that FXa is a particularly attractive target for the development of oral antithrombotic agents. In view of the excellent pharmaceutical properties of 1,2-phenylenediamine-based FXa inhibitors and the reported structure-activity relationship (SAR) analysis of FXa inhibitors, we designed and synthesized a series of 3,4-diaminobenzoyl-based FXa inhibitors. Intensive SAR studies on this new series led to the discovery of 3,4-dimethoxyl substituted compound 7b. 7b is a highly potent, selective, direct FXa inhibitor with excellent in vivo antithrombotic activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Yang J,Su G,Ren Y,Chen Y

doi

10.1016/j.ejmech.2015.06.012

subject

Has Abstract

pub_date

2015-08-28 00:00:00

pages

41-51

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30088-X

journal_volume

101

pub_type

杂志文章

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