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
来源：
CHEMICAL BIOLOGY & DRUG DESIGN | 2009年 / 73卷 / 01期
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.
引用
收藏
页码：142 / 146
页数：5
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