[Synthesis of N-alpha-(arylsulfonylglycyl)amidinophenylalanine amides as highly active inhibitors of thrombin].
The headline compounds were prepared from purified cyanophenylalanines after presenting arylsulfonylglycyl residues, activation of the carboxyl group by formation of the p- nitrophenylester followed by aminolysis and transfer of a cyano in an amidine function. Besides some esters and an acid were synthetized with the basic structure mentioned in the headline . The p-compounds with a cycloaliphatic amide component proved as "tight binding inhibitors". The greatest antithrombin effect shows N alpha-(2- naphthylsulphonylglycyl )-4- amidinophenylalaninpiperidi d with a Ki-value of 6 X 10(-9) mol/l using S-2238 as a substrate.
D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013917:Thrombin / Q000037:antagonists & inhibitors*
D010649:Phenylalanine; D013917:Thrombin
Synthese von N alpha-(Arylsulfonylglycyl)amidinophenylalaninamiden als hochaktive Inhibitoren des Thrombins.