| 摘要 |
Novel N-formyl hydroxylamine derivatives are provided to inhibit growth of Streptococcus pneumoniae and antibiotic-resistant bacteria by inhibiting activity of peptide deformylase(PDF) associated with protein biosynthesis and polypeptide maturation, thereby treating respiratory disease. The N-formyl hydroxylamine derivatives represented by the formula(I) are provided, wherein A is -C(=O)NHOH or -N(CHO)OH; R1 is hydrogen, C1-3 alkyl, C4-6 cycloalkyl, halogen or hydroxyl; R2 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkenyl, C4-6 cycloalkyl, N or O-containing C4-6 heterocycle or benzyl; R3 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkenyl, C4-6 cycloalkyl, phenyl or benzyl; Y is a compound represented by the formula(IIa) or formula(IIb). In the formula(IIa) or formula(IIb), R4 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkenyl, C4-6 cycloalkyl, phenyl or benzyl; and R5 is hydrogen, halogen, amino, C1-6 alkyl substituted amino, aryl substituted amino, furan or a compound represented by the formula(III). In the formula(III), R6-R10 is independently hydrogen, linear or branched C1-3 alkyl, linear or branched halogen substituted C1-4 alkyl, hydroxy, acyl, acyloxy, halogen(fluoro, chloro, bromo, iodo), cyano, nitro, amino, N,N-dimethylamino, phenyl, morpholinyl or formyl.
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