Inhibition of trypsin, plasmin, thrombin and kallikrein by various esters of guanidino- and amidino-acids.
Inhibitory effects of various phenolic esters of trans-4-guanidinomethylcyclohexanecarboxylic acid, amidino-piperidine-4-alkanoic acids or trans-4-amidinocyclohexane-4-alkanoic acids on trypsin, thrombin, plasmin and pancreatic kallikrein were examined. Their inhibitory effects were strongly affected by the acid portion and phenolic group constituting the esters. The effects of the acidic portion and phenolic group on the inhibitory effect varied with each protease; they were most effective on thrombin and plasmin and least effective on kallikrein. The inhibitory effect of these esters on trypsin was affected mainly by acid portion.
Faculty of Pharmacy, Tokushima Bunri University, Japan.
H
H
Akashi
T
T
Ariki
M
M
Kato
Y
Y
Kozaki
T
T
Irisawa
M
M
Muramatu
D000578:Amidines / Q000494:pharmacology*; D000595:Amino Acid Sequence; D003509:Cyclohexanecarboxylic Acids / Q000494:pharmacology*; D003510:Cyclohexanes / Q000494:pharmacology*; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D006801:Humans; D007610:Kallikreins / Q000037:antagonists & inhibitors; D008969:Molecular Sequence Data; D010179:Pancreas / Q000201:enzymology; D010880:Piperidines / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000494:pharmacology*; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000494:pharmacology
D000578:Amidines; D003509:Cyclohexanecarboxylic Acids; D003510:Cyclohexanes; D010880:Piperidines; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; C038303:NCO 650; D007610:Kallikreins; D013917:Thrombin; D005341:Fibrinolysin