- Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis
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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.
- Lu, Tianbao,Markotan, Thomas,Coppo, Frank,Tomczuk, Bruce,Crysler, Carl,Eisennagel, Stephen,Spurlino, John,Gremminger, Lisa,Soll, Richard M.,Giardino, Edward C.,Bone, Roger
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p. 3727 - 3731
(2007/10/03)
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- Cyclic oxyguanidine protease inhibitors
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Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or pharmaceuticall
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