| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366072 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
SAR about the B-ring of a series of N2-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1′ and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
Graphical abstractSAR about the B-ring of N2-aroyl anthranilamide 3e is described. B-ring o-aminoalkylethers and B-ring p-amine probes of the S1′ and S4 sites, respectively, afforded picomolar factor Xa and nanomolar factor IIa inhibitors that were potent in in vitro anticoagulation assays.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
David Mendel, Angela L. Marquart, Sajan Joseph, Philip Waid, Ying K. Yee, Anne Louise Tebbe, Andrew M. Ratz, David K. Herron, Theodore Goodson, John J. Masters, Jeffry B. Franciskovich, Jennifer M. Tinsley, Michael R. Wiley, Leonard C. Weir,