Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.

@article{Huang2003DesignSA,
  title={Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.},
  author={Wenrong Huang and M. A. Naughton and Hua Yang and Ting Yu Su and Suiko Dam and Paul W Wong and Ann Arfsten and Susan Edwards and Uma Sinha and Stanley Hollenbach and Robert M. Scarborough and Bing-yan Zhu},
  journal={Bioorganic & medicinal chemistry letters},
  year={2003},
  volume={13 4},
  pages={
          723-8
        }
}
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 IC(50) below 1 nM against factor Xa. 

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