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ID: ALA1138120

Journal: Bioorg Med Chem Lett

Title: Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.

Authors: Young WB, Sprengeler P, Shrader WD, Li Y, Rai R, Verner E, Jenkins T, Fatheree P, Kolesnikov A, Janc JW, Cregar L, Elrod K, Katz B.

Abstract: Inhibition of coagulation proteases such as thrombin, fXa, and fVIIa has been a focus of ongoing research to produce safe and effective antithrombotic agents. Herein, we describe a unique zinc-mediated chelation strategy to streamline the discovery of potent inhibitors of fIIa, fXa, and fVIIa. SAR studies that led to the development of selective inhibitors of fXa will also be detailed.

CiteXplore: 16257204

DOI: 10.1016/j.bmcl.2005.10.023