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PDBsum entry 1t4u
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Hydrolase/hydrolase inhibitor
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PDB id
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1t4u
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References listed in PDB file
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Key reference
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Title
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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
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T.Lu,
T.Markotan,
F.Coppo,
B.Tomczuk,
C.Crysler,
S.Eisennagel,
J.Spurlino,
L.Gremminger,
R.M.Soll,
E.C.Giardino,
R.Bone.
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Ref.
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Bioorg Med Chem Lett, 2004,
14,
3727-3731.
[DOI no: ]
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PubMed id
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Abstract
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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.
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