Oxyguanidines. Part 2: discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis

…, B Tomczuk, C Crysler, S Eisennagel, J Spurlino…

文献索引：Lu, Tianbao; Markotan, Thomas; Coppo, Frank; Tomczuk, Bruce; Crysler, Carl; Eisennagel, Stephen; Spurlino, John; Gremminger, Lisa; Soll, Richard M.; Giardino, Edward C.; Bone, Roger Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 14 p. 3727 - 3731

全文：HTML全文

被引用次数: 19

摘要

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.