Stürzebecher J, Horn H, Markwardt F, Wagner G, Walsmann P
Pharmazie. 1981 Sep;36(9):639-41.
Amides of N alpha-substituted 3-amidinophenylalanine are potent inhibitors of the serine proteinases trypsin, plasmin and thrombin. They belong to the most potent inhibitors of these enzymes of the benzamidine type. In contrast, amides of 4-amidinophenylalanine possess weak inhibitory activity towards trypsin and plasmin. The cyclic amides of this group, however, are potent thrombin inhibitors. These derivatives are the first benzamidines with specific antithrombin activity. The isomeric compounds of 3-amidinophenyl-3-aminopropionic acids possess weak inhibitory effects on trypsin, plasmin and thrombin.
Nα-取代的3-脒基苯丙氨酸的酰胺是丝氨酸蛋白酶胰蛋白酶、纤溶酶和凝血酶的有效抑制剂。它们属于苯甲脒类中这些酶的最有效抑制剂。相比之下，4-脒基苯丙氨酸的酰胺对胰蛋白酶和纤溶酶具有较弱的抑制活性。然而，该基团的环状酰胺是有效的凝血酶抑制剂。这些衍生物是首批具有特异性抗凝血酶活性的苯甲脒。3-脒基苯基-3-氨基丙酸的异构体化合物对胰蛋白酶、纤溶酶和凝血酶具有较弱的抑制作用。
