[Synthetic serine proteinase inhibitors. 30. Synthesis of alpha-benzoylamino-4-amidinocinnamic acid and alpha-(4-amidinobenzoylamino) cinnamic acid amides, and their inhibitory effect on trypsin-like enzymes].
To test their inhibitory activity against enzymes, the authors synthetized the compounds named in the title. The synthesis started from the corresponding azlactones 1 and 9. Subsequent aminolysis led to the alpha-benzoyl-aminocinnamic acid amides 2 and 10 which contain a cyano function. The acid amides were converted, in different ways, to the desired amidine salts 4, 7, 12 and 15. The amidines obtained showed but little inhibitory activity against the serine proteinases thrombin, trypsin and plasmin.
D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D002934:Cinnamates / Q000138:chemical synthesis* / Q000494:pharmacology; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D011480:Protease Inhibitors; D012697:Serine Endopeptidases; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000138:chemical synthesis
D000577:Amides; D002934:Cinnamates; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; D012697:Serine Endopeptidases; D013917:Thrombin; D005341:Fibrinolysin
Synthetische Inhibitoren der Serinproteinasen. 30. Mitteilung: Synthese von alpha-Benzoylamino-4-amidinozimtsäureamiden sowie alpha-(4-Amidinobenzoylamino)zimtsäureamiden und ihre Hemmwirkung gegenüber trypsinähnlichen Enzymen.