Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.
Article Details
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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
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.
Bioorg Med Chem Lett. 2006 Feb;16(3):710-3. Epub 2005 Oct 27.
- PubMed ID
- 16257204 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Hemi-Babim Prothrombin Ki (nM) 1 N/A N/A Details Hemi-Babim Prothrombin Ki (nM) 70000 N/A N/A Details