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厚朴酚类类似物作为口腔细菌抑制剂

Honokiol-Inspired Analogs as Inhibitors of Oral Bacteria.

作者信息

Solinski Amy E, Ochoa Cristian, Lee Young Eun, Paniak Thomas, Kozlowski Marisa C, Wuest William M

机构信息

Department of Chemistry, 1515 Dickey Drive, Emory University , Atlanta, Georgia 30322, United States.

Department of Chemistry, Roy and Diana Vagelos Laboratories, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.

出版信息

ACS Infect Dis. 2018 Feb 9;4(2):118-122. doi: 10.1021/acsinfecdis.7b00178. Epub 2017 Dec 13.

Abstract

The oral microbiome is a complex ecological niche where both commensal and pathogenic bacteria coexist. Previous reports have cited that the plant isolate honokiol is a potent inhibitor of S. mutans biofilms. Herein we report a cross-coupling method that provides access to a concise library of honokiol-inspired analogs. Through this work we determined that the inhibitory activity of honokiol is highly dependent on the growth conditions. Further, we identify a series of analogs that display significant potency against oral bacteria leading to the discovery of a potent antimicrobial.

摘要

口腔微生物群是一个复杂的生态位,共生细菌和致病细菌共存于此。先前的报道称,植物提取物厚朴酚是变形链球菌生物膜的有效抑制剂。在此,我们报告一种交叉偶联方法,可用于构建一个简洁的厚朴酚类似物文库。通过这项工作,我们确定厚朴酚的抑制活性高度依赖于生长条件。此外,我们鉴定出一系列对口腔细菌具有显著效力的类似物,从而发现了一种强效抗菌剂。

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