New synthetic inhibitors of C1r, C1 esterase, thrombin, plasmin, kallikrein and trypsin.
p-Guanidinobenzoate derivates were prepared and their inhibitory effects on trypsin, plasmin, pancreatic kallikrein, plasma kallikrein, thrombin, C1r and C1 esterase were examined. Among the various inhibitors tested, 6'-amidino-2-naphthyl-4-guanidinobenzoate dihydrochloride, 4-(beta-amidinoethenyl)phenyl-4-guanidinobenzoate dimethanesulfonate and 4-amidino-2-benzoylphenyl-4-guanidinobenzoate dimethanesulfonate were the most effective inhibitors of trypsin, plasmin, pancreatic kallikrein. plasma kallikrein and thrombin and they strongly inhibited the esterolytic activities of C1r and C1 esterase, and then strongly inhibited complement-mediated hemolysis.
D001550:Benzamidines; D003166:Complement Activating Enzymes / Q000037:antagonists & inhibitors; D003174:Complement C1 Inactivator Proteins; D015923:Complement C1r; D004792:Enzyme Precursors / Q000037:antagonists & inhibitors; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D006146:Guanidines / Q000494:pharmacology*; D006801:Humans; D007610:Kallikreins / Q000037:antagonists & inhibitors; D011480:Protease Inhibitors / Q000494:pharmacology*; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000494:pharmacology
D001550:Benzamidines; D003174:Complement C1 Inactivator Proteins; D004792:Enzyme Precursors; D006146:Guanidines; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; C032857:4-(beta-amidinoethenyl)phenyl-4-guanidinobenzoate dimethanesulfonate; C032856:4-amidino-2-benzoylphenyl 4-guanidinobenzoate dimethanesulfonate; D003166:Complement Activating Enzymes; D007610:Kallikreins; D015923:Complement C1r; D013917:Thrombin; D005341:Fibrinolysin; C032855:nafamostat