Author/Authors :
Zhaozhong J. Jia، نويسنده , , Yanhong Wu، نويسنده , , Wenrong Huang، نويسنده , , Erick Goldman، نويسنده , , Penglie Zhang، نويسنده , , John Woolfrey، نويسنده , , Paul Wong، نويسنده , , Brian Huang، نويسنده , , Uma Sinha، نويسنده , , Gary Park، نويسنده , , Andrea Reed، نويسنده , , Robert M. Scarborough، نويسنده , , Bing-Yan Zhu، نويسنده ,
Abstract :
Based on DuPont Pharmaceuticalsʹ monobenzamidine lead structure SN429, we have designed the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as a novel series of non-basic factor Xa inhibitors. We have discovered that the displacement of the benzamidine moiety with substituted 2-naphthyl structures not only results in highly potent factor Xa inhibitors, but also significantly increases their enzyme specificity and oral bioavailability.
