| 摘要 |
Compounds possessing novel P1 amino acid replacements of the formulae (I) or (II) where R<1> is a peptidic or peptidomimetic recognition sequence P2-Pn targeting the S2- Sn pockets of HCV NS-3 serine protease, where n is 3-6, which recognition sequence is peptide bonded to formula (I); R<2> is H, C1-C3 alkyl; R<3> is C1-C3 alkyl, optionally substituted with 1-3 halo atoms or -SH; R<4> is =O, halo, amino or -OH; R<5> is C1-C6 alkyl, C0-C3-alkylaryl, C0-C3-alkylhet, C0-C3-alkylcycloC3-C6-alkyl, any of which can be optionally substituted with hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 alkoxy C1-C6 alkyl, C1-C6 alkanoyl, amino, halo, carboxy, cyano, azido, mercapto, nitro, C0-C3-alkylaryl, C0-C3-alkylhet, C0-C3-alkylcycloalkyl; R<6> is H C1-C3 alkyl or cyclises with the nominal N-terminal to form a macrocycle; with the proviso that if R4 is =O, then the alkyl moiety of R5 as alkylaryl or alkylhet is C1-C3 alkanyl or C2-C3 alkenyl; have utility as HCV NS-3 serine protease inhibitors. |
