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. 1989 Nov;37(11):3108-11.
doi: 10.1248/cpb.37.3108.

Synthesis of tripeptide chloromethyl ketones and examination of their inhibitory effects on plasmin and plasma kallikrein

Y Tsuda, N Teno, Y Okada, K Wanaka, M Bohgaki, A Hijikata-Okunomiya, U Okamoto, T Naito, S Okamoto
Free article

Synthesis of tripeptide chloromethyl ketones and examination of their inhibitory effects on plasmin and plasma kallikrein

Y Tsuda et al. Chem Pharm Bull (Tokyo). 1989 Nov.
Free article

Abstract

With the aim of obtaining selective synthetic inhibitors of plasmin and plasma kallikrein, D-Ile-Phe-Lys-CH2Cl, Ile-Phe-Lys-CH2Cl, D-Ile-Phe-Arg-CH2Cl and Ile-Phe-Arg-CH2Cl were synthesized and their inhibitory activity against plasmin, plasma kallikrein and other trypsin-like serine proteinases was examined. Among them, D-Ile-Phe-Arg-CH2Cl exhibited a highly selective inhibitory activity against plasma kallikrein, yet D-Ile-Phe-Lys-CH2Cl exhibited nearly the same order of inhibitory activity against plasmin as well as plasma kallikrein.

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