From antimicrobial activity to mechanism of resistance: the multifaceted role of simple quaternary ammonium compounds in bacterial eradication

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• 作者：Kevin P.C. Minbiole^a ; ^{kevin.minbiole@villanova.edu" class="auth_mail" title="E-mail the corresponding author} ; Megan C. Jennings^b ; Laura E. Ator^a ; Jacob W. Black^a ; Melissa C. Grenier^a ; Jade E. LaDow^c ; Kevin L. Caran^d ; Kyle Seifert^c ; William M. Wuest^b ;
• 关键词：Quaternary ammonium compound ; Antibacterial ; Antibiofilm ; Amphiphile ; MultiQAC
• 刊名：Tetrahedron
• 出版年：2016
• 出版时间：23 June 2016
• 年：2016
• 卷：72
• 期：25
• 页码：3559-3566
• 全文大小：722 K

文摘

Quaternary ammonium compounds (QACs) are a prominent class of antibacterial agents. Drawing inspiration from commercial disinfectants and antimicrobial natural products, we have derivatized structurally diverse tertiary amines to generate several different classes of QACs. We have synthesized over 200 QACs, many of which exhibit potent antibacterial and antibiofilm activity. Analysis of the structure–activity relationship of our compounds have led to the facile production of inexpensive QACs that display ∼1 μM MIC against a suite of bacteria, and furthermore do not appear to trigger bacterial resistance systems in methicillin-resistant Staphylococcus aureus (MRSA).