Synthesis and Structure-Activity Study of Protease Inhibitors. V.Chemical Modification of 6-Amidino-2-naphthyl 4-Guanidinobenzoate

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By developing 6-amidino-2-naphthyl 4-guanidinobenzoate (I, FUT-175) as a basic structure, its various derivatives were synthesized and their inhibitory activities on trypsin, plasmin, kallikrein, thrombin, C1^^- and C1s^^- as well as on complement-mediated hemolysis were examined. The protective effect of these compounds on complement-mediated Forssman shock was also examined in guinea pigs. 6-Amidino-2-naphthyl 4-[(4,5-dihydro-1H-imidazol-2-yl)amino]-benzoate (41,FUT-187) was found to be a suitable compound for oral administration with anti-complement activity superior to that of compound I.
社団法人日本薬学会の論文
1993-01-15