Synthesis and structure-activity relationship study of the new set of trypsin-like proteinase inhibitors

P Zlatoidsky, T Maliar

Index: Zlatoidsky, Pavol; Maliar, Tibor European Journal of Medicinal Chemistry, 1999 , vol. 34, # 12 p. 1023 - 1034

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Citation Number: 15

Abstract

Anew set of 25 trypsin-like proteinase inhibitors was prepared and the inhibiting activity on trypsin, thrombin, plasmin and urokinase was measured. The structure-activity relationship is discussed. High inhibiting activities were observed in 4-guanidinobenzoic acid esters only. The replacement of this moiety for N-formamidinyl-isonipecotic acid or an arginine moiety caused almost total loss of the activity. In the series of 4-guanidinobenzoic acid esters, any ...