[Synthetic inhibitors of serine proteinases. 35. Inhibition action of amidino- and guanidinophenyl derivatives against hemolysis initiated by complement activation].
Selected amidino- and guanidinophenyl derivatives which have already proved to be inhibitors of serine proteinases were tested on their inhibitory effect on complement activation. To quantitate the inhibitory action the decreasing rate of haemolysis of sensitized sheep erythrocytes was recorded continuously. Compounds exerting a more or less pronounced inhibitory effect on trypsin-like proteinases turned out to have a corresponding inhibitory influence on complement-mediated haemolysis. The inhibitory effect of some amidinobenzyliden derivatives on the complement activity was markedly higher than could be expected from their general antiproteolytic efficacy. Changing the basic structure into amidinophenyl amino acid amides with strong and selective antithrombin effect completely abolished the inhibitory influence on complement.
Hoffmann
A
A
Institut für Pharmakologie und Toxikologie der Medizinischen Akademie Erfurt.
Markwardt
F
F
D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D003167:Complement Activation / Q000187:drug effects*; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006461:Hemolysis / Q000187:drug effects*; D066298:In Vitro Techniques; D011817:Rabbits; D015842:Serine Proteinase Inhibitors; D012756:Sheep
D000578:Amidines; D006146:Guanidines; D015842:Serine Proteinase Inhibitors
Synthetische Inhibitoren der Serinproteinasen. 35. Mitteilung: Uber die Hemmwirkung von Amidino- und Guanidinophenyl-Derivaten auf die durch Komplementaktivierung ausgelöste Hämolyse.