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Bioorg Med Chem Lett. 2003 Feb 24;13(4):723-8.

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

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Department of Medicinal Chemistry, Millennium Pharmaceuticals Inc., 256 East Grand Ave., South San Francisco, CA 94080, USA.


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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