Synthesis and structure-activity study of protease inhibitors. I. (Guanidinophenyl)propionate and guanidinocinnamate derivatives.

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Abstract
Guanidino-ester derivatives were synthesized and evaluated for inhibitory activities against trypsin, plasmin, kallikrein, thrombin and Cl esterase, as well as on in vitro complement-mediated hemolysis. Among the compounds synthesized, phenyl-.alpha.-ethyl-p-guanidinocinnamate (IVg) and phenyl .alpha.-propyl-p-guanidinocinnamate (IVh) exhibited potent and selective Cl esterase inhibition (IC50 [median inhibitory concentration]: 7 .times. 10-6 and 6 .times. 10-6 M, respectively) and 6-methyl-3-pyridyl-.alpha.-ethyl-p-guanidinocinnamate (IVi) markedly suppressed complement-mediated hemolysis (86% inhibition at 1 .times. 10-3 M).