Synthesis and structure-activity study of protease inhibitors. II. Amino- and guanidino-substituted naphthoates and tetrahydronaphthoates.

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Abstract
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-I-naphthoate and phenyl 6-guanidino-1-naphthoate exhibited potent and selective trypsin inhibition (IC50 [median inhibitory concentration] 4 .times. 10-7 and 5 .times. 10-8 M, respectively) and phenyl 7-guanidino-1,2,3,4-tetrahydro-1-naphthoate and p-ethoxycarbonylphenyl 7-guanidino-1,2,3,4-tetrahydro-1-naphthoate had selective inhibitory activities against thrombin (IC50: 4 .times. 10-5 and 1 .times. 10-5 M, respectively).

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