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  • Title: [Analysis of the relationship between the reactivity of synthetic substrates and thrombin inhibitors and their structure].
    Author: Kibirev VK, Gershkovich AA, Serebrianyĭ SB.
    Journal: Ukr Biokhim Zh (1978); 1983; 55(3):271-6. PubMed ID: 6868150.
    Abstract:
    Kinetics of thrombin- and trypsin-catalyzed hydrolysis of diphenylacetyl-L-arginine esters was studied at pH 8.5 and 25 degrees C, and the antithrombin activity of in vitro synthesized compounds was examined. The anticlotting activity of arylsulphonyl-L-arginine methyl esters appeared to be higher than that of the derivatives of diphenyl arginine. Relations were found connecting polar (delta) and steric (Es) characteristics of substituent (R) in R-C6H4-SO2-Arg-OCH3 esters with their antithrombin activity in vitro or with efficiency of their thrombin-catalyzed hydrolysis. This gives supplementary possibilities for synthesis of new substrates and more potent thrombin inhibitors.
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