214911-32-7Relevant academic research and scientific papers
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors
Huang, Wenrong,Naughton, Mary Ann,Yang, Hua,Su, Ting,Dam, Suiko,Wong, Paul W.,Arfsten, Ann,Edwards, Susan,Sinha, Uma,Hollenbach, Stanley,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 723 - 728 (2007/10/03)
A series of novel transition state factor Xa inhibitors containing a variety of lactam ring systems as central templates was synthesized in an expedient manner and allowed for a great deal of structural variability. Among them, the piperazinone-based inhibitors were found to be not only active against factor Xa but also selective over thrombin. Optimization of the P4 moiety yielded several potent compounds with IC50 below 1 nM against factor Xa.
Selective factor Xa inhibitors
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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.
