| 摘要 |
Compounds of the general formula I are provided:and pharmaceutically acceptable salts thereof, wherein,Z is a chemical species or Ri capable of binding at a primary specificity site of a protease;Y is a chemical species reactive to a specific class of protease;each of R2, R3, R5 and R7 is independently selected from the group consisting hydrogen, alkyls, aryls, substituted aryls, alkylaryls and arylalkyls;R4 and R6 are independently selected from the group consisting of:(a) H, alkyl, aryl, arylalkyl, alkylaryl, substituted derivatives thereof, and Ri;(b) -C(O)OH and derivatives thereof, said derivatives selected from the group consisting of -C(O)OQ, -C(O)NRYRZ, -C(O)[NHCHRi(q)C(O)]qOQ, and -C(O)[NHCHRi(q)C(O)]qNRYRZ; and(c) -CHRiNH2 and derivatives thereof, said derivatives selected from the group consisting of -CHRiNHW, -CHRiNHC(O)OQ, -CHRiNHC(O)R, -CHRiNHC(O)NRYRZ, -CHRiNHC(O)[NHCHRi(q)C(O)]qOQ, -CHRiNHSO2R, and -CHRiNH[C(O)CHRi(r)NH]rW, where q and r independently are integers from 1 to 10 inclusive; J is a carboxyl protecting group; G is an amino protecting group; Q is H, R or J; W is H, R or G; each Ri is independently selected from naturally or non-naturally occurring amino acid side chains; R is alkyl, aryl, substituted aryl, alkylaryl, arylalkyl, or heterocyclic radical; and each RY and RZ is independently H, alkyl, aryl, substituted aryl, alkylaryl, arylalkyl, or heterocyclic radical.
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