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A Bisphenolic Honokiol Analog Outcompetes Oral Antimicrobial Agent Cetylpyridinium Chloride via a Membrane-Associated Mechanism.
ACS Infectious Diseases ( IF 5.3 ) Pub Date : 2019-11-12 , DOI: 10.1021/acsinfecdis.9b00190
Cristian Ochoa 1 , Amy E Solinski 2 , Marcus Nowlan 1 , Madeline M Dekarske 2 , William M Wuest 2 , Marisa C Kozlowski 1
Affiliation  

Targeting Streptococcus mutans is the primary focus in reducing dental caries, one of the most common maladies in the world. Previously, our groups discovered a potent bactericidal biaryl compound that was inspired by the natural product honokiol. Herein, a structure activity relationship (SAR) study to ascertain structural motifs key to inhibition is outlined. Furthermore, mechanism studies show that bacterial membrane disruption is central to the bacterial growth inhibition. During this process, it was discovered that analog C2 demonstrated a 4-fold better therapeutic index compared to the commercially available antimicrobial cetylpyridinium chloride (CPC) making it a viable alternative for oral care.

中文翻译:

双酚厚朴酚类似物通过膜相关机制胜过口服抗菌剂氯化十六烷基吡啶鎓。

靶向变形链球菌是减少龋齿的主要重点,龋齿是世界上最常见的疾病之一。以前,我们的小组发现了一种受自然产物厚朴酚启发的有效的杀菌联芳基化合物。在此,概述了确定抑制关键的结构基序的结构活性关系(SAR)研究。此外,机理研究表明细菌膜破坏是抑制细菌生长的关键。在此过程中,发现与市售的抗菌十六烷基吡啶鎓氯化物(CPC)相比,类似物C2的治疗指数高4倍,使其成为口腔护理的可行替代品。
更新日期:2019-11-13
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