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本文引用的文献

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Retapamulin: an antibacterial with a novel mode of action in an age of emerging resistance to Staphylococcus aureus.瑞他帕林:在对金黄色葡萄球菌耐药性不断出现的时代,一种具有新型作用模式的抗菌药物。
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The pleuromutilin antibiotics: a new class for human use.截短侧耳素类抗生素:一类供人类使用的新型抗生素。
Curr Opin Investig Drugs. 2010 Feb;11(2):182-91.
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Comparative evaluation of epidemiology and outcomes of methicillin-resistant Staphylococcus aureus (MRSA) USA300 infections causing community- and healthcare-associated infections.耐甲氧西林金黄色葡萄球菌(MRSA)USA300感染导致社区和医疗保健相关感染的流行病学及转归的比较评估
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Severe surgical site infection in community hospitals: epidemiology, key procedures, and the changing prevalence of methicillin-resistant Staphylococcus aureus.社区医院中的严重手术部位感染:流行病学、关键手术及耐甲氧西林金黄色葡萄球菌的流行变化
Infect Control Hosp Epidemiol. 2007 Sep;28(9):1047-53. doi: 10.1086/520731. Epub 2007 Jul 12.
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Update to the multiplex PCR strategy for assignment of mec element types in Staphylococcus aureus.金黄色葡萄球菌中mec元件类型分类的多重PCR策略更新
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Antibiotic Substances From Basidiomycetes: VIII. Pleurotus Multilus (Fr.) Sacc. and Pleurotus Passeckerianus Pilat.担子菌纲的抗生素物质:VIII. 糙皮侧耳(平菇)(弗里斯)萨卡尔。和佛罗里达侧耳菌皮拉特。
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Interaction of pleuromutilin derivatives with the ribosomal peptidyl transferase center.截短侧耳素衍生物与核糖体肽基转移酶中心的相互作用。
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Practice guidelines for the diagnosis and management of skin and soft-tissue infections.皮肤及软组织感染诊断和管理的实践指南。
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9
Inhibition of peptide bond formation by pleuromutilins: the structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin.截短侧耳素对肽键形成的抑制作用:嗜放射栖热菌50S核糖体亚基与替米考星复合物的结构
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研究性截短侧耳素化合物 BC-3781 针对与急性细菌性皮肤和皮肤结构感染相关的常见革兰氏阳性菌的抗菌活性。

Antimicrobial activity of the investigational pleuromutilin compound BC-3781 tested against Gram-positive organisms commonly associated with acute bacterial skin and skin structure infections.

机构信息

JMI Laboratories, North Liberty, Iowa, USA.

出版信息

Antimicrob Agents Chemother. 2012 Mar;56(3):1619-23. doi: 10.1128/AAC.05789-11. Epub 2012 Jan 9.

DOI:10.1128/AAC.05789-11
PMID:22232289
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3294907/
Abstract

BC-3781 is a novel semisynthetic pleuromutilin antimicrobial agent developed as an intravenous and oral therapy for acute bacterial skin and skin structure infections (ABSSSI) and respiratory tract infections (RTI). BC-3781 and comparator agents were tested by the broth microdilution method against 1,893 clinical Gram-positive organisms predominantly causing ABSSSI. BC-3781 exhibited potent activity against methicillin-resistant Staphylococcus aureus (MIC(50/90), 0.12/0.25 μg/ml), coagulase-negative staphylococci (MIC(50/90), 0.06/0.12 μg/ml), β-hemolytic streptococci (MIC(50/90), 0.03/0.06 μg/ml), viridans group streptococci (MIC(50/90), 0.12/0.5 μg/ml), and Enterococcus faecium (including vancomycin-nonsusceptible strains) (MIC(50/90), 0.12/2 μg/ml). Compared with other antibiotics in use for the treatment of ABSSSI, BC-3781 displayed the lowest MICs and only a minimal potential for cross-resistance with other antimicrobial classes.

摘要

BC-3781 是一种新型半合成截短侧耳素类抗菌药物,开发用于治疗急性细菌性皮肤和皮肤结构感染(ABSSSI)和呼吸道感染(RTI)的静脉内和口服治疗药物。BC-3781 和对照药物通过肉汤微量稀释法对 1893 种主要引起 ABSSSI 的临床革兰氏阳性菌进行了测试。BC-3781 对耐甲氧西林金黄色葡萄球菌(MIC(50/90),0.12/0.25μg/ml)、凝固酶阴性葡萄球菌(MIC(50/90),0.06/0.12μg/ml)、β-溶血性链球菌(MIC(50/90),0.03/0.06μg/ml)、草绿色链球菌(MIC(50/90),0.12/0.5μg/ml)和屎肠球菌(包括万古霉素耐药株)(MIC(50/90),0.12/2μg/ml)具有强大的活性。与用于治疗 ABSSSI 的其他抗生素相比,BC-3781 显示出最低的 MIC 值,并且与其他抗菌药物类别仅具有最小的交叉耐药潜力。