6-peptidylamino-1-naphthalenesulfonamides useful as fluorogenic proteolytic enzyme substrates

摘要

The present invention encompasses compounds of formula I: I and the pharmaceutically acceptable non-toxic salts thereof; wherein R1 is hydrogen, lower alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, or phenylalkyl; R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, or phenylalkyl; or NR1R2 forms a nitrogen heterocycle; and R3 is hydrogen, an amino acid or a peptide residue. These compounds may be employed as substrates in assays for determining proteolytic enzyme activity or as enzyme inhibitors. The invention also encompasses methods for determining proteolytic enzyme activity using the compounds of formula I.