- Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors
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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.
- 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
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p. 723 - 728
(2007/10/03)
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- Complexes possessing ortho ligating functionality
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A group of functionalized amine chelants having ortho ligating functionality that form complexes with rare-earth type metal ions are disclosed. The chelants possess the general formula STR1 wherein R'1, R'2, R'3, R'4, R'5 and R'6, Z' and X are all defined in the specification. In addition certain of the chelant-radionuclide complexes can be effectively employed in compositions useful as therapeutic and/or diagnostic agents for calcific tumors and/or relief of bone pain.
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