Membrane-Active Antibacterial Agents Based on Calix[4]arene Derivatives: Synthesis and Biological Evaluation

Bacteria have developed increasing resistance to currently used antimicrobial agents. New classes of antimicrobial drugs are urgently required to fight drug-resistant pathogens. Here, we designed and synthesized a series of calix[4]arene derivatives as antibacterial agents by biomimicking the struct...

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Veröffentlicht in:Frontiers in chemistry 2022-02, Vol.10, p.816741-816741
Hauptverfasser: Fang, Shanfang, Dang, Yuan-Ye, Li, Haizhou, Li, Hongxia, Liu, Jiayong, Zhong, Rongcui, Chen, Yongzhi, Liu, Shouping, Lin, Shuimu
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Sprache:eng
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Zusammenfassung:Bacteria have developed increasing resistance to currently used antimicrobial agents. New classes of antimicrobial drugs are urgently required to fight drug-resistant pathogens. Here, we designed and synthesized a series of calix[4]arene derivatives as antibacterial agents by biomimicking the structural properties and biological functions of antibacterial peptides. After introducing cationic hydrophilic moieties and preliminary structural optimization, we obtained a lead compound ( ) that exhibited excellent antibacterial activity against Gram-positive bacteria, low toxicity toward mammalian cells and poor hemolytic activity. The antibacterial mechanism studies showed that compound can destroy bacterial cell membrane directly, leading to bacterial death and a low tendency to develop bacterial resistance.
ISSN:2296-2646
2296-2646
DOI:10.3389/fchem.2022.816741