[Synthetic inhibitors of serine proteinases. 31. The inhibition of trypsin, plasmin and thrombin by isomeric compounds of N alpha -arylsulfonylated omega-amidinophenyl-alpha-aminoalkylcarboxylic acid amides].
Isomeric compounds of N alpha-arylsulfonylated amides of omega-amidinophenyl-alpha-aminoalkylcarboxylic acids--N alpha-amidinophenylsulfonylated amides or N alpha-arylsulfonylated amidino anilides of omega-phenyl-alpha-aminoalkylcarboxylic acids, respectively--possess weak antithrombin activity as compared to the derivatives of the basic structure. Thus, the assumption is corroborated that specific enzyme-inhibitor interactions account for the high antithrombin activity of certain derivatives of omega-amidinophenyl-alpha-aminoalkylcarboxylic acids. In contrast, amidinoanilides of N alpha-substituted omega-phenyl-alpha-aminoalkylcarboxylic acids are potent inhibitors of trypsin and plasmin, their inhibitory activity approaches that of primary amides of N alpha-substituted omega-amidinophenyl-alpha-aminoalkylcarboxylic acids.
D000578:Amidines / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D006801:Humans; D007536:Isomerism; D011480:Protease Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013451:Sulfonic Acids / Q000494:pharmacology*; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000494:pharmacology
D000578:Amidines; D011480:Protease Inhibitors; D013451:Sulfonic Acids; D014361:Trypsin Inhibitors; D013917:Thrombin; D005341:Fibrinolysin
Synthetische Inhibitoren der Serinproteinasen. 31. Mitteilung: Uber die Hemmwirkung isomerer Verbindungen von N alpha-arylsulfonylierten omega-Amidinophenyl-alpha-aminoalkylcarbonsäureamiden gegenüber Trypsin, Plasmin und Thrombin.