Ochoa Cristian, Solinski Amy E, Nowlan Marcus, Dekarske Madeline M, Wuest William M, Kozlowski Marisa C
Department of Chemistry, Roy and Diana Vagelos Laboratories , University of Pennsylvania , 231 South 34th Street , Philadelphia , Pennsylvania 19104 , United States.
Department of Chemistry and the Emory Antibiotic Resistance Center , Emory University , 1515 Dickey Drive , Atlanta , Georgia 30322 , United States.
ACS Infect Dis. 2020 Jan 10;6(1):74-79. doi: 10.1021/acsinfecdis.9b00190. Epub 2019 Nov 12.
Targeting 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 demonstrated a 4-fold better therapeutic index compared to the commercially available antimicrobial cetylpyridinium chloride (CPC) making it a viable alternative for oral care.
靶向治疗是减少龋齿的主要关注点，龋齿是世界上最常见的疾病之一。此前，我们的团队发现了一种受天然产物厚朴酚启发的强效杀菌联芳基化合物。本文概述了一项结构活性关系（SAR）研究，以确定抑制作用的关键结构基序。此外，机制研究表明，细菌膜破坏是细菌生长抑制的核心。在此过程中，发现该类似物的治疗指数比市售抗菌剂西吡氯铵（CPC）高4倍，使其成为口腔护理的可行替代品。
