[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].
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.
Voigt
B
B
Sektion Biowissenschaften der Karl-Marx-Universität Leipzig, Lehrstuhl Pharmazeutische Chemie.
Stürzebecher
J
J
Wagner
G
G
Markwardt
F
F
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
D004151:Dipeptides; D009842:Oligopeptides; D015842:Serine Proteinase Inhibitors; D014361:Trypsin Inhibitors; D013917:Thrombin; D005341:Fibrinolysin
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.