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[Synthetic inhibitors of serine proteinases. Part 26: Inhibition of trypsin, plasmin and thrombin by amides of N alpha-arylsulfonylated 2-amino-4-(4-amidino-phenyl) butyric acid and 2-amino-5-amidinophenyl valeric acids (author's transl)]. 1982

J Stürzebecher, and F Markwardt, and H Vieweg, and G Wagner, and P Walsmann

Among the derivatives of the N alpha-arylsulfonylated omega-amidinophenyl-alpha-aminoalkyl carboxylic acids, the primary amides of N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl) butyric acid proved to be compounds with strong antiplasmin and antitrypsin activity, they exert, however, only slight inhibitory effect on thrombin. So far, no benzamidine derivatives with strong inhibitory effects on plasmin but with weak antithrombin activity have been known. The secondary amides of the N alpha-arylsulfonylated 2-amino-4-(4-amidinophenyl)butyric acid possess slight inhibitory effects, the corresponding derivatives of 2-amino-5-amidinophenyl valeric acids, however, are potent inhibitors of thrombin.

UI MeSH Term Description Entries
D010654 Phenylbutyrates Derivatives of 4-phenylbutyric acid, including its salts and esters.
D011480 Protease Inhibitors Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES). Antiprotease,Endopeptidase Inhibitor,Endopeptidase Inhibitors,Peptidase Inhibitor,Peptidase Inhibitors,Peptide Hydrolase Inhibitor,Peptide Hydrolase Inhibitors,Peptide Peptidohydrolase Inhibitor,Peptide Peptidohydrolase Inhibitors,Protease Antagonist,Protease Antagonists,Antiproteases,Protease Inhibitor,Antagonist, Protease,Antagonists, Protease,Hydrolase Inhibitor, Peptide,Hydrolase Inhibitors, Peptide,Inhibitor, Endopeptidase,Inhibitor, Peptidase,Inhibitor, Peptide Hydrolase,Inhibitor, Peptide Peptidohydrolase,Inhibitor, Protease,Inhibitors, Endopeptidase,Inhibitors, Peptidase,Inhibitors, Peptide Hydrolase,Inhibitors, Peptide Peptidohydrolase,Inhibitors, Protease,Peptidohydrolase Inhibitor, Peptide,Peptidohydrolase Inhibitors, Peptide
D005341 Fibrinolysin A product of the lysis of plasminogen (profibrinolysin) by PLASMINOGEN activators. It is composed of two polypeptide chains, light (B) and heavy (A), with a molecular weight of 75,000. It is the major proteolytic enzyme involved in blood clot retraction or the lysis of fibrin and quickly inactivated by antiplasmins. Plasmin,Fibrogammin,Glu-Plasmin,Protease F,Thrombolysin,Glu Plasmin
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000578 Amidines Derivatives of oxoacids RnE(
D013917 Thrombin An enzyme formed from PROTHROMBIN that converts FIBRINOGEN to FIBRIN. Thrombase,Thrombin JMI,Thrombin-JMI,Thrombinar,Thrombostat,alpha-Thrombin,beta,gamma-Thrombin,beta-Thrombin,gamma-Thrombin,JMI, Thrombin
D014361 Trypsin Inhibitors Serine proteinase inhibitors which inhibit trypsin. They may be endogenous or exogenous compounds. Trypsin Inhibitor,Inhibitor, Trypsin,Inhibitors, Trypsin

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