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

AI Article Synopsis

Article 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.

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Source
http://dx.doi.org/10.1016/s0960-894x(02)01037-5DOI Listing

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