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棘霉素类抗生素对耐多药及形成生物膜的金黄色葡萄球菌和粪肠球菌的构效关系研究

Structure-activity studies of echinomycin antibiotics against drug-resistant and biofilm-forming Staphylococcus aureus and Enterococcus faecalis.

作者信息

Socha Aaron M, Laplante Kerry L, Russell David J, Rowley David C

机构信息

Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA.

出版信息

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1504-7. doi: 10.1016/j.bmcl.2009.01.010. Epub 2009 Jan 10.

DOI:10.1016/j.bmcl.2009.01.010
PMID:19185486
Abstract

Four echinomycin antibiotics were isolated from the culture broth of a marine streptomycete, and their structures were determined by a combination of chemical and spectroscopic analyses. Antibiotic activities were measured against drug-resistant and biofilm-forming strains of Staphylococcus aureus and Enterococcus faecalis. Minimum inhibitory concentrations ranging from 0.01 microM to greater than 14 microM clearly defined structure-activity relationships for antibiotic potency. Echinomycin was the most active compound with a MIC of 0.03 microM against methicillin-resistant S. aureus and 0.01 microM against biofilm-forming E. faecalis.

摘要

从一株海洋链霉菌的培养液中分离出了四种棘霉素类抗生素,其结构通过化学分析和光谱分析相结合的方法得以确定。测定了这些抗生素对金黄色葡萄球菌和粪肠球菌的耐药菌株及形成生物膜菌株的抗菌活性。最低抑菌浓度范围为0.01微摩尔至大于14微摩尔,清晰地界定了抗生素效力的构效关系。棘霉素是活性最强的化合物,对耐甲氧西林金黄色葡萄球菌的最低抑菌浓度为0.03微摩尔,对形成生物膜的粪肠球菌的最低抑菌浓度为0.01微摩尔。

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