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    Bioorg Med Chem Lett. 2004 Jul 16;14(14):3727-31.

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

    Lu T, Markotan T, Coppo F, Tomczuk B, Crysler C, Eisennagel S, Spurlino J, Gremminger L, Soll RM, Giardino EC, Bone R.

    3-Dimensional Pharmaceuticals, Inc., 665 Stockton Drive, Exton, PA 19341, USA. tlu3@prdus.jnj.com

    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.

    PMID: 15203151 [PubMed - indexed for MEDLINE]

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