[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.