330803-77-5Relevant articles and documents
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P1 structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides
Jia, Zhaozhong J.,Wu, Yanhong,Huang, Wenrong,Goldman, Erick,Zhang, Penglie,Woolfrey, John,Wong, Paul,Huang, Brian,Sinha, Uma,Park, Gary,Reed, Andrea,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 1651 - 1655 (2007/10/03)
Based on DuPont Pharmaceuticals' 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.
