714249-01-1Relevant academic research and scientific papers
Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity
Koshio, Hiroyuki,Hirayama, Fukushi,Ishihara, Tsukasa,Taniuchi, Yuta,Sato, Kazuo,Sakai-Moritani, Yumiko,Kaku, Seiji,Kawasaki, Tomihisa,Matsumoto, Yuzo,Sakamoto, Shuichi,Tsukamoto, Shin-Ichi
, p. 2179 - 2191 (2004)
Factor Xa (fXa) is a serine protease involved in the coagulation cascade, which has received great interest as a potential target for the development of new antithrombotic drugs. Herein we report a novel series of fXa inhibitors in which the 1,4-diazepane moiety was designed to interact with the S4 aryl-binding domain of the fXa active site. Compound 13 (YM-96765) showed potent fXa inhibitory activity (IC50=6.8nM) and effective antithrombotic activity without prolonging bleeding time.
