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  • Title: Thrombin inhibitors. 1. Ester derivatives of N alpha-(arylsulfonyl)-L-arginine.
    Author: Okamoto S, Kinjo K, Hijikata A, Kikumoto R, Tamao Y, Ohkubo K, Tonomura S.
    Journal: J Med Chem; 1980 Aug; 23(8):827-30. PubMed ID: 7401109.
    Abstract:
    A series of N alpha-(arylsulfonyl)-L-arginine esters was prepared and tested as inhibitors of the clotting activity of thrombin. N alpha-Dansyl-L-arginine methyl ester was the most inhibitory of the N alpha-(arylsulfonyl)-L-arginine methyl esters. The most potent inhibitors were the n-propyl and n-butyl esters of N alpha-dansyl-L-arginine with an I50 of 2 X 10(-6) M. Esters of unsaturated straight-chain alcohols with a chain length of four carbons were also as inhibitory as the n-butyl ester. The inhibitors were hydrolyzed by thrombin and trypsin more slowly than N alpha-tosyl-L-arginine methyl ester.
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