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Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis |
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| Authors: | Lu Tianbao Markotan Thomas Coppo Frank Tomczuk Bruce Crysler Carl Eisennagel Stephen Spurlino John Gremminger Lisa Soll Richard M Giardino Edward C Bone Roger |
| Institution: | 3-Dimensional Pharmaceuticals, Inc., 665 Stockton Drive, Exton, PA 19341, USA. tlu3@prdus.jnj.com |
| Abstract: | Through structure-based drug design and parallel synthesis, we have discovered a novel series of nonpeptidic phenyl-based thrombin inhibitors using oxyguanidines as guanidine bioisosteres. These compounds have been found to be highly potent, highly selective, and orally bioavailable. |
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