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吡咯并吡唑基取代恶唑烷酮RWJ-416457的体外抗菌活性

In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.

作者信息

Foleno Barbara D, Abbanat Darren, Goldschmidt Raul M, Flamm Robert K, Paget Steve D, Webb Glenda C, Wira Ellyn, Macielag Mark J, Bush Karen

机构信息

Johnson and Johnson Pharmaceutical Research and Development, L.L.C., Raritan, NJ 08869, USA.

出版信息

Antimicrob Agents Chemother. 2007 Jan;51(1):361-5. doi: 10.1128/AAC.01017-06. Epub 2006 Nov 13.

DOI:10.1128/AAC.01017-06
PMID:17101672
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1797661/
Abstract

RWJ-416457, an investigational pyrrolopyrazolyl-substituted oxazolidinone, inhibited the growth of linezolid-susceptible staphylococci, enterococci, and streptococci at concentrations of < or =4 microg/ml, generally exhibiting two- to fourfold-greater potency than that of linezolid. Time-kill studies demonstrated bacteriostatic effects for both RWJ-416457 and linezolid.

摘要

RWJ - 416457是一种正在研究的吡咯并吡唑基取代的恶唑烷酮，在浓度≤4微克/毫升时可抑制对利奈唑胺敏感的葡萄球菌、肠球菌和链球菌的生长，其效力通常比利奈唑胺强2至4倍。时间杀菌研究表明RWJ - 416457和利奈唑胺均有抑菌作用。

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本文引用的文献

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The emergence of infections with community-associated methicillin resistant Staphylococcus aureus.社区获得性耐甲氧西林金黄色葡萄球菌感染的出现。
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Oxazolidinone structure-activity relationships leading to linezolid.导致利奈唑胺的恶唑烷酮结构-活性关系。
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Linezolid in vitro: mechanism and antibacterial spectrum.利奈唑胺的体外作用机制及抗菌谱
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Cross-linking in the living cell locates the site of action of oxazolidinone antibiotics.活细胞中的交联定位了恶唑烷酮类抗生素的作用位点。
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Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions.恶唑烷酮类药物的作用机制：利奈唑胺和依哌唑胺对翻译反应的影响。
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