679427-01-1Relevant academic research and scientific papers
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity
Zhang, Penglie,Bao, Liang,Zuckett, Jingmei F.,Jia, Zhaozhong J.,Woolfrey, John,Arfsten, Ann,Edwards, Susan,Sinha, Uma,Hutchaleelaha, Athiwat,Lambing, Joseph L.,Hollenbach, Stanley J.,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 989 - 993 (2007/10/03)
Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa inhibitors with substituted biphenyl P4 groups. Structure-activity relationship studies around 2 have led to a series of potent factor Xa inhibitors which are highly active in the human plasma-based thrombin generation assay with 2XTG values less than 1 μM. Compound 55 shows strong antithrombotic activity in our rabbit deep vein thrombosis model, and also exhibits good oral bioavailability and a long half life in rats.
