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ID: ALA1136598
Journal: Bioorg Med Chem Lett
Title: Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.
Authors: Huang W, Naughton MA, Yang H, Su T, Dam S, Wong PW, Arfsten A, Edwards S, Sinha U, Hollenbach S, Scarborough RM, Zhu BY.
Abstract: 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.
CiteXplore: 12639567