[Synthesis of N-alpha-(8-quinolinesulfonyl)-4-amidinophenylalanine amides as thrombin inhibitors].
The compounds mentioned in the title were prepared starting from 4-cyanophenylalanine by sulfonylation using 8-quinoline sulfonic acid chloride, formation of the 4-nitrophenylester, aminolysis of the latter and subsequent transformation of the cyano via the thiocarbamoyl and the thioimid acid ester into the amidine group. The antithrombin effect decreased by substituting the 1-naphthylsulfonyl by the 8-quinolinesulfonyl residue.
D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013917:Thrombin / Q000037:antagonists & inhibitors*
D011804:Quinolines; D010649:Phenylalanine; D013917:Thrombin
Synthese von N alpha-(8-Chinolinsulfonyl)-4-amidinophenylalaninamiden als Thrombininhibitoren.