| 摘要 |
A compound having the Formula I, wherein: X is CH, N, or CQ1, with the proviso that when X is CQ1, at least one of Q or Q1 is H; R is H, alkyl, arylalkyl, heteroalkyl, heteroarylalkyl, alkoxyalkyl, a side chain of a naturally occurring amino acid, or (CH2)n NH-L, the alkyl, arylalkyl, heteroalkyl, or heteroarylalkyl groups being optionally substituted; R1 is H, halogen, cyano, nitro, -S(.=O)2 OH, hydroxyl, alkyl, alkoxy, hydroxymethyl, alkoxymethyl, arylalkyl, carboxyl, alkoxycarbonyl, alkylcarbonyloxy, haloalkyl, N(RR3), or acyl; Q is H, lower alkyl, cycloalkyl, hydroxyl, alkoxy, halogen, arylalkyl, arylalkeny, arylalkynyl, aryl, heteroaryl, heteroalkyl, cycloalkyl, S-R, S(.=O)R, S(.=O)2 R, N(RR3), or NHS(.=O)2 R, the arylalkyl, arylalkenyl, arylalkynyl, aryl, heteroaryl, and heteroalkyl groups being optionally substituted; Q1 is the same as Q; Z is COCONH-R7 ; R7 is K, -A-N(R8)-G, -O-A-N(R8)-G, -A-SO2 N(R8) (R9), or -O-A-SO2 N(R8) (R9); K is alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, heteroaryl, aryl, arylalkyl, heterocycloalkyl, alkoxy, alkoxyalkyl, arylalkyloxy, or N(RR3), the K groups being optionally substituted; With the proviso that when R7 is K, then Q is selected from the group consisting of optionally substituted arylalkenyl and optionally substituted arylalkynyl; and with the further proviso that when K is alkyl, then X is not CH when Q is optionally substituted arylalkynyl; Also described as a composition for inhibiting a serine protease or a cysteine protease comprising the compound described above and a pharmaceutically acceptable carrier. The compound of formula I is useful for inhibiting a serine protease or cysteine protease.
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