Title of article
4-Amidinobenzylamine-Based inhibitors of urokinase
Author/Authors
Sebastian Künzel، نويسنده , , Andrea Schweinitz، نويسنده , , Siegmund Rei?mann، نويسنده , , J?rg Stürzebecher، نويسنده , , Torsten Steinmetzer، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
4
From page
645
To page
648
Abstract
A series of 4-amidinobenzylamine-based peptidomimetic inhibitors of urokinase was synthesized. The most potent one, benzylsulfonyl- -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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792037
Link To Document