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  • Title: Protease-inhibitory activities of leupeptin analogues.
    Author: Saino T, Someno T, Ishii S, Aoyagi T, Umezawa H.
    Journal: J Antibiot (Tokyo); 1988 Feb; 41(2):220-5. PubMed ID: 2965694.
    Abstract:
    Thirty analogues of leupeptin were synthesized and examined for their inhibitory activities against trypsin, papain, plasmin, kallikrein, thrombin and urokinase in vitro. Benzoyl- and alpha-naphthalenesulfonyl-L-leucyl-L-argininal were 8 times more inhibitory to papain, benzyloxycarbonyl-L-pyroglutamyl-L-leucyl-L-argininal 10 times more to trypsin and plasmin, and DL-2-pipecolyl-L-leucyl-L-argininal 25 times more to kallikrein than leupeptin. Against urokinase, only L-pyroglutamyl-L-leucyl-L-argininal exhibited a potent inhibitory activity. alpha-Naphthalensulfonyl-, dansyl- and benzyloxycarbonyl-(2S,3R)-3-amino-2-hydroxy-4-phenylbutyryl-L-leucyl-L- argininal were inhibitory to thrombin.
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