Synthesis and Structure-Activity Study of Protease Inhibitors. II. Amino-and Guanidino-Substituted Naphthoates and Tetrahydronaphthoates

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Various amino-and guanidino-substituted naphthoates and tetrahydronaphthoates were synthesized and evaluated for inhibitory activities against trypsin, plasmin, kallikrein, thrombin and Cl esterase. Among these compounds, phenyl 4-guanidino-1-naphthoate (IIIj) and phenyl 6-guanidino-1-naphthoate (IIIl) exhibited potent and selective trypsin inhibition (IC_<50> : 4×10^<-7> and 5×10^<-8> M, respectively) and phenyl 7-guanidino-1,2,3,4-tetrahydro-1-naphthoate (Vb) and p-ethoxycarbonylphenyl 7-guanidino-1,2,3,4-tetrahydro-1-naphthoate (Vg) had selective inhibitory activities against thrombin (IC_<50> : 4×10^<-5> and 1×10^<-5> M, respectively).
社団法人日本薬学会の論文
1984-10-25