84228-43-3Relevant articles and documents
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors
Yang, Jiabin,Su, Guoqiang,Ren, Yu,Chen, Yang
, p. 41 - 51 (2015/06/30)
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 structureeactivity 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.