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新型恶唑烷-2-酮类似物对耐甲氧西林金黄色葡萄球菌菌株的抗菌活性

Antibacterial activity of new oxazolidin-2-one analogues in methicillin-resistant Staphylococcus aureus strains.

作者信息

Córdova-Guerrero Jesús, Hernández-Guevara Esteban, Ramírez-Zatarain Sandy, Núñez-Bautista Marco, Ochoa-Terán Adrián, Muñiz-Salazar Raquel, Montes-Ávila Julio, López-Angulo Gabriela, Paniagua-Michel Armando, Torres Gustavo A Nuño

机构信息

Escuela de Ciencias de la Salud, Universidad Autónoma de Baja California, Ensenada, Baja California 22890, Mexico.

Centro de Graduados e Investigación en Química, Instituto Tecnológico de Tijuana, Tijuana, Baja California 22000, Mexico.

出版信息

Int J Mol Sci. 2014 Mar 26;15(4):5277-91. doi: 10.3390/ijms15045277.

DOI:10.3390/ijms15045277
PMID:24675696
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4013563/
Abstract

Staphylococcus aureus is one of the most common causes of nosocomial infections. The purpose of this study was the synthesis and in vitro evaluation of antimicrobial activity of 10 new 3-oxazolidin-2-one analogues on 12 methicillin resistant S. aureus (MRSA) clinical isolates. S. aureus confirmation was achieved via catalase and coagulase test. Molecular characterization of MRSA was performed by amplification of the mecA gene. Antimicrobial susceptibility was evaluated via the Kirby-Bauer disc diffusion susceptibility test protocol, using commonly applied antibiotics and the oxazolidinone analogues. Only (R)-5-((S)-1-dibenzylaminoethyl)-1,3-oxazolidin-2-one (7a) exhibited antibacterial activity at 6.6 μg. These results, allow us to infer that molecules such as 7a can be potentially used to treat infections caused by MRSA strains.

摘要

金黄色葡萄球菌是医院感染最常见的病因之一。本研究的目的是合成10种新的3-恶唑烷-2-酮类似物,并对其针对12株耐甲氧西林金黄色葡萄球菌(MRSA)临床分离株的抗菌活性进行体外评估。通过过氧化氢酶和凝固酶试验确认金黄色葡萄球菌。通过扩增mecA基因对MRSA进行分子特征分析。使用常用抗生素和恶唑烷酮类似物,通过 Kirby-Bauer 纸片扩散药敏试验方案评估抗菌药敏性。只有(R)-5-((S)-1-二苄基氨基乙基)-1,3-恶唑烷-2-酮(7a)在6.6μg时表现出抗菌活性。这些结果使我们推断,诸如化合物7a这样的分子可能可用于治疗由MRSA菌株引起的感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/a6554aad5d96/ijms-15-05277f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/044026937350/ijms-15-05277f1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/a6554aad5d96/ijms-15-05277f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/044026937350/ijms-15-05277f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/9d50c5a38dd9/ijms-15-05277f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/bd3c0adb2750/ijms-15-05277f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/584d6207eb60/ijms-15-05277f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/33d493b9fd54/ijms-15-05277f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c262/4013563/a6554aad5d96/ijms-15-05277f6.jpg

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本文引用的文献

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MEGA5: molecular evolutionary genetics analysis using maximum likelihood, evolutionary distance, and maximum parsimony methods.MEGA5:用于最大似然法、进化距离法和最大简约法的分子进化遗传学分析。
Mol Biol Evol. 2011 Oct;28(10):2731-9. doi: 10.1093/molbev/msr121. Epub 2011 May 4.
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Genomic variation and evolution of Staphylococcus aureus.金黄色葡萄球菌的基因组变异与进化。
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Use of an automated multiple-locus, variable-number tandem repeat-based method for rapid and high-throughput genotyping of Staphylococcus aureus isolates.使用基于多位点可变数目串联重复序列的自动化方法对金黄色葡萄球菌分离株进行快速高通量基因分型。
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Novel Mannich ketones of oxazolidinones as antibacterial agents.新型恶唑烷酮类曼尼希酮作为抗菌剂
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