AUTHOR=Fang Shanfang , Dang Yuan-Ye , Li Haizhou , Li Hongxia , Liu Jiayong , Zhong Rongcui , Chen Yongzhi , Liu Shouping , Lin Shuimu 

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

JOURNAL=Frontiers in Chemistry

VOLUME=10

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.816741

DOI=10.3389/fchem.2022.816741

ISSN=2296-2646

ABSTRACT=<p>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 (<bold>16</bold>) 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 <bold>16</bold> can destroy bacterial cell membrane directly, leading to bacterial death and a low tendency to develop bacterial resistance.</p>