600707-97-9Relevant articles and documents
4-Amidinobenzylamine-Based Inhibitors of Urokinase
Kuenzel, Sebastian,Schweinitz, andrea,Reissmann, Siegmund,Stuerzebecher, Joerg,Steinmetzer, Torsten
, p. 644 - 648 (2007/10/03)
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 Ki 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.