[Synthetic inhibitors of serine proteinases. Part 19: On the inhibitory effect of amidinobenzylidene derivatives of benzo-condensed cycloalkanones on trypsin, plasmin and thrombin (author's transl)].
Amidinobenzylidene derivatives of benzo-condensed cycloalkanones proved to be potent competitive inhibitors of thrombin and trypsin. On the contrary, the antiplasmin effect of these derivatives is considerably less marked. The conversion of 3-amidinochalcone to derivatives in which the carbonyl group is incorporated into a ring, does not lead to fundamental changes in the inhibitory effect on trypsin and thrombin, whereas the antiplasmin effect decreases. Compared to 4-amidinochalcone, the 2-(4-amidinobenzylidene) derivatives of indanone-(1) and tetralone-(1) exert a stronger inhibitory effect on trypsin and thrombin. The introduction of a hetero-atom to the cycloalkanone component affected the inhibitory effect on trypsin and thrombin but insignificantly. From these results it is concluded that also in amidinobenzylidene derivatives of benzo-condensed cycloalkanone derivatives, the carbonyl function shares in enzyme-inhibitor binding.
D001597:Benzylidene Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D005341:Fibrinolysin / Q000037:antagonists & inhibitors*; D006801:Humans; D013917:Thrombin / Q000037:antagonists & inhibitors*; D014361:Trypsin Inhibitors / Q000138:chemical synthesis
D001597:Benzylidene Compounds; D014361:Trypsin Inhibitors; D013917:Thrombin; D005341:Fibrinolysin
Synthetische Inhibitoren der Serinproteinasen. 19. Mitteilung: Uber die Hemmwirkung von Amidinobenzylidenderivaten benzokondensierter Cycloalkanone auf Trypsin, Plasmin und Thrombin.