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

Toyoo NAKAYAMA; Seizo TAIRA; Masato IKEDA; Hiroshi ASHIZAWA; Minoru ODA; Katsumasa ARAKAWA; Setsuro FUJII

doi:10.1248/cpb.41.117

中山豊男, 平良盛三, 池田昌人, 芦澤広, 織田実, 荒川勝雅, 藤井節郎

著者情報

キーワード: protease inhibition, C1r^^-, C1s^^-, anti-complement activity, Forssman shock, amidinonaphthol, structure-activity relationship

ジャーナルフリー

1993 年 41 巻 1 号 p. 117-125

DOI https://doi.org/10.1248/cpb.41.117

詳細

抄録

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.

責任著者(Corresponding author)

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