Saino T, Someno T, Ishii S, Aoyagi T, Umezawa H
Research Laboratories, Pharmaceuticals Group, Nippon Kayaku Co., Ltd., Tokyo, Japan.
J Antibiot (Tokyo). 1988 Feb;41(2):220-5. doi: 10.7164/antibiotics.41.220.
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.
