title: [Synthesis of N-alpha-(arylsulfonyl)-4-amidino-phenylalanyl-prolines and N-alpha-(arylsulfonylglycyl)-4-amidino-phenylalanyl-prolines and testing of them as inhibitors of serine proteinases. 33. Synthetic inhibitors of serine proteinases].
abstract: The headline compounds were prepared by the reaction of N alpha-(arylsulfonyl)- and N alpha-(arylsulfonylglycyl)-4-cyanophenylalanines to the L- and D-proline derivatives. These compounds were transformed in a usual manner in the amidino compounds. The substitution of the pyrrolidine residue by L-proline in this type of inhibitors decreased the activity against serine proteases, especially against thrombin. In the case of the D-proline derivatives the decrease of the inhibitor activity against thrombin was very high.
authors.affiliation: Sektion Biowissenschaften der Karl-Marx-Universität Leipzig, Lehrstuhl Pharmazeutische Chemie.
authors.forename: B
authors.initials: B
authors.lastname: Voigt
authors.forename: J
authors.initials: J
authors.lastname: Stürzebecher
authors.forename: G
authors.initials: G
authors.lastname: Wagner
authors.forename: F
authors.initials: F
authors.lastname: Markwardt
mesh_terms: D055598:Chemical Phenomena; D002621:Chemistry; D004151:Dipeptides / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D015842:Serine Proteinase Inhibitors; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors
chemical_list: D004151:Dipeptides; D009842:Oligopeptides; D015842:Serine Proteinase Inhibitors; D014361:Trypsin Inhibitors; D013917:Thrombin; D005341:Fibrinolysin
vernacular_title: Synthese von N alpha-(Arylsulfonyl)-4-amidino-phenylalanyl-prolinen und von N alpha-(Arylsulfonylglycyl)-4-amidino-phenylalanyl-prolinen und deren Prüfung als Inhibitoren von Serinproteinasen. 33. Mitteilung: Synthetische Inhibitoren der Serinproteinasen.