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Synthesis and In Vitro Antibacterial Activity of (2S)-N-(Substitutedphenyl)-1-[(2R)-2-[(Formylhydroxyamino)Methyl]-1-Oxohexyl]-2-Pyrrolidinecarboxamides as Potential Peptide Deformylase Inhibitors
被引:3
|作者:
Wang, Zhenyu
[1
]
Zhou, Weicheng
[1
]
机构:
[1] Shanghai Inst Pharmaceut Ind, State Key Lab New Drug & Pharmaceut Proc, Shanghai 200437, Peoples R China
关键词:
antibacterial agent;
Gram-positive bacteria;
inhibitor;
peptide deformylase;
NVP PDF-713;
TARGET;
ACID;
D O I:
10.1111/j.1747-0285.2008.00753.x
中图分类号:
Q5 [生物化学];
Q7 [分子生物学];
学科分类号:
071010 ;
081704 ;
摘要:
Gram-positive organisms have re-emerged as the major hospital pathogens, which make the unmet medical needs for antibacterial therapy even worse. In searching for potent agents against Gram-positive pathogens, novel (2S)-N-(substitutedphenyl)-1-[(2R)-2-[(formylhydroxyamino)methyl]-1-oxohexyl]-2-pyrrolidinecarboxamides, analogues of peptide deformylase inhibitor LBM-415 were designed, synthesized and evaluated for their antibacterial activities in vitro. Many of these compounds exhibited high potency against Gram-positive organisms compared with reference agent: LBM-415.
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页码:142 / 146
页数:5
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