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西莫环菌素 D8 在临床环境中对革兰氏阴性菌起作用。

Simocyclinone D8 turns on against Gram-negative bacteria in a clinical setting.

机构信息

Department of Histology, Microbiology and Medical Biotechnologies, University of Padova, via Gabelli 63, 35121 Padova, Italy.

出版信息

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1202-4. doi: 10.1016/j.bmcl.2009.11.135. Epub 2009 Dec 4.

DOI:10.1016/j.bmcl.2009.11.135
PMID:20022496
Abstract

Simocyclinone D8 (SD8) is known to affect Gram-positive bacteria only. By testing SD8 against several clinical isolates, we showed that SD8 resulted very active against Gram-negative bacteria from clinical specimens, while it was shown inactive against laboratory strains. The activity against the former was in part due to enhanced drug entry. In addition, SD8 appears to share chromosome- and plasmid-mediated resistance mechanisms with fluoroquinolones.

摘要

西莫环酮 D8(SD8)已知仅对革兰氏阳性菌有影响。通过对几种临床分离株进行 SD8 测试,我们发现 SD8 对来自临床标本的革兰氏阴性菌非常有效,而对实验室菌株则无效。对前者的活性部分归因于增强的药物进入。此外,SD8 似乎与氟喹诺酮类药物具有染色体和质粒介导的耐药机制。

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Exploiting bacterial DNA gyrase as a drug target: current state and perspectives.利用细菌 DNA 拓扑异构酶作为药物靶点:现状与展望。
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