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Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1:
C K Marlowe1, U Sinha, A C Gunn
1COR Therapeutics, Inc., South San Francisco, CA 94080, USA.
Bioorganic & Medicinal Chemistry Letters
|January 15, 2000
Abstract:
A series of arginine aldehyde inhibitors was designed as transition state (TS) analogues based on the known factor Xa specific substrate Cbz-D-Arg-Gly-Arg-pNA. BnSO2-(D)Arg-Gly-Arg-H (20) was found to be the most potent and selective inhibitor of factor Xa and prothrombinase activity in this series.