[Synthetic inhibitors of serine proteinases. Part 26: Inhibition of trypsin, plasmin and thrombin by amides of N alpha-arylsulfonylated 2-amino-4-(4-amidino-phenyl) butyric acid and 2-amino-5-amidinophenyl valeric acids (author's transl)].
Among the derivatives of the N alpha-arylsulfonylated omega-amidinophenyl-alpha-aminoalkyl carboxylic acids, the primary amides of N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl) butyric acid proved to be compounds with strong antiplasmin and antitrypsin activity, they exert, however, only slight inhibitory effect on thrombin. So far, no benzamidine derivatives with strong inhibitory effects on plasmin but with weak antithrombin activity have been known. The secondary amides of the N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl)butyric acid possess slight inhibitory effects, the corresponding derivatives of 2-amino-5-amidinophenyl valeric acids, however, are potent inhibitors of thrombin.
D000578:Amidines / Q000494:pharmacology*; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D006801:Humans; D010654:Phenylbutyrates / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000494:pharmacology*; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000494:pharmacology
D000578:Amidines; D010654:Phenylbutyrates; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; D013917:Thrombin; D005341:Fibrinolysin
Synthetische Inhibitoren der Serinproteinasen. 26. Mitteilung 2: Hemmung von Trypsin, Plasmin und Thrombin durch Amide N alpha-arylsulfonylierter 2-Amino-4-(4-amidinophenyl)buttersäure und 2-Amino-5-amidinophenylvaleriansäuren.