[Synthesis of N alpha-(arylsulfonylglycylglycyl)-4-amidinophenylalanine amides as thrombin inhibitors].
The headline compounds were prepared using N-arylsulfonylglycylglycine-4-nitrophenyl esters. Firstly these compounds were aminolized with 4-cyanphenyl alanine and thereby the N alpha-(arylsulfonylglycylglycyl)-4-cyanphenyl alanines got were transferred into the 4-nitrophenyl esters After aminolysis the desired hydroiodides of the headline compounds starting from the cyano compounds were prepared via the carbamoyl compounds and the thiomidic acid methyl ester hydroiodides. The arylsulfonylglycylglycine rest caused a decreasing of the inhibitor activity.
D000578:Amidines / Q000138:chemical synthesis; D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D066298:In Vitro Techniques; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013451:Sulfonic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D013917:Thrombin / Q000037:antagonists & inhibitors*
D000578:Amidines; D013451:Sulfonic Acids; D010649:Phenylalanine; D013917:Thrombin
Synthese von N alpha-(Arylsulfonylglycylglycyl)-4-amidinophenylalaninamiden als Thrombininhibitoren.