262299-33-2Relevant articles and documents
Synthesis and structure-activity relationship study of the new set of trypsin-like proteinase inhibitors
Zlatoidsky, Pavol,Maliar, Tibor
, p. 1023 - 1034 (2007/10/03)
A new 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 important influence of the ester-groups reactivity was observed. The trypsin-thrombin selectivity in the compounds with the guanidine-remote carboxylic function was also observed.