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ID: ALA1135855
Journal: Bioorg Med Chem Lett
Title: 4-amidinobenzylamine-based inhibitors of urokinase.
Authors: Künzel S, Schweinitz A, Reissmann S, Stürzebecher J, Steinmetzer T.
Abstract: A series of 4-amidinobenzylamine-based peptidomimetic inhibitors of urokinase was synthesized. The most potent one, benzylsulfonyl-D-Ser-Ala-4-amidinobenzylamide 16, inhibits uPA with a K(i) of 7.7 nM but is less selective than 10 with a Gly as P2 residue. Hydroxyamidine and carbonate prodrugs were prepared, which are rapidly converted into the active inhibitors in rats after subcutaneous application.
CiteXplore: 11844691