476352-82-6Relevant academic research and scientific papers
Inhibitors of factor Xa
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, (2008/06/13)
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors
Zhang, Penglie,Zuckett, Jingmei F.,Woolfrey, John,Tran, Katherine,Huang, Brian,Wong, Paul,Sinha, Uma,Park, Gary,Reed, Andrea,Malinowski, John,Hollenbach, Stan,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 1657 - 1661 (2007/10/03)
Monoamidine FXa inhibitors 3 were designed and synthesized. SAR studies and molecular modeling led to the design of conformationally constrained diaryl ethers 4 and 5, as well as benzopyrrolidinone 7 as potent FXa inhibitors. The monoamidines show high efficacy in a DVT model, but lack desirable oral bioavailability. The benzopyrrolidinone-based aminoisoquinolines 8 do not show significant improvement in oral bioavailability.
