Synthetic inhibitors of trypsin, plasmin, kallikrein, thrombin, C1r-, and C1 esterase.
p-Carbethoxyphenyl episol-guanidinocaproate and p-(p'-guanidinobenzoyloxy)-phenyl derivatives were prepared, and their inhibitory effects on trypsin, plasmin, plasma kallikrein, thrombin, C1r- and C1 esterase were examined. Among the various inhibitors tested, p-nitrophenyl p'-guanidinobenzoate, N,N-dimethylamino p-(p'-guanidinobenzoyloxy)-benzoyl glycolate and N,N-dimethylamino p-(p'-guanidinobenzoyloxy)-benzilcarbonyloxy glycolate were the most effective inhibitors of trypsin, plasmin, plasma kallikrien and thrombin, and they strongly inhibited the esterolytic activities of C1r- and C1 esterase.
D003166:Complement Activating Enzymes / Q000037:antagonists & inhibitors*; D003174:Complement C1 Inactivator Proteins / Q000138:chemical synthesis; D005341:Fibrinolysin / Q000037:antagonists & inhibitors*; D006146:Guanidines / Q000494:pharmacology; D007610:Kallikreins / Q000037:antagonists & inhibitors*; D007700:Kinetics; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors*; D014361:Trypsin Inhibitors / Q000138:chemical synthesis
D003174:Complement C1 Inactivator Proteins; D006146:Guanidines; D014361:Trypsin Inhibitors; D003166:Complement Activating Enzymes; D007610:Kallikreins; D013917:Thrombin; D005341:Fibrinolysin