INHIBITION OF TRYPSIN, PLASMIN, THROMBIN AND KALLIKREIN BY VARIOUS ESTERS OF GUANIDINO-ACIDS AND AMIDINO-ACIDS

Inhibitory effects of various phenolic esters of trans-4-guanidinometh ylcyclohexanecarboxylic acid, amidinopiperidine-4-alkanoic acids or tr ans-4-amidinocyclohexane-4-alkanoic acids on trypsin, thrombin, plasmi n and pancreatic kallikrein were examined. Their inhibitory effects we re strongly affected by the acid portion and phenolic group constituti ng the esters. The effects of the acidic portion and phenolic group on the inhibitory effect varied with each protease; they were most effec tive on thrombin and plasmin and least effective on kallikrein. The in hibitory effect of these esters on trypsin was affected mainly by acid portion.