Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 243, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2022.114765
Keywords
Quaternary ammonium compounds; Antibacterial; Structure -activity relationships; Mechanism
Categories
Funding
- National Natural Science Foundation of China
- Shandong Provin- cial Natural Science Foundation
- [82003595]
- [ZR2020QH346]
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This review summarizes the chemical diversity, structure-activity relationships, and antibacterial mechanisms of quaternary ammonium compounds (QACs) reported over the past decade. The review aims to provide sufficient information for medicinal chemists to discover new generation antibacterial agents based on QACs.
Bacterial infections have seriously threatened public health especially with the increasing resistance and the clifflike decline of the number of newly approved antibacterial agents. Quaternary ammonium compounds (QACs) possess potent medicinal properties with 95 successfully marketed drugs, which also have a long history as antibacterial agents. In this review, we summarize the chemical diversity of antibacterial QACs, divided into chain-like and aromatic ring, reported over the past decade (2012 to mid-2022). Additionally, the structureactivity relationships, mainly covering hydrophobicity, charges and skeleton features, are discussed. In the cases where sufficient information is available, antibacterial mechanisms including biofilm, cell membrane, and intracellular targets are presented. It is hoped that this review will provide sufficient information for medicinal chemists to discover the new generation of antibacterial agents based on QACs.
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