Thiazolopyrimidinone Derivative H5–23 Enhances Daptomycin Activity against Linezolid-Resistant <i>Enterococcus faecalis</i> by Disrupting the Cell Membrane

Xiong, Yanpeng; Chen, Zhong; Bai, Bing; Peng, Yalan; Liu, Shanghong; Fang, Di; Wen, Zewen; Shang, Yongpeng; Lin, Zhiwei; Han, Shiqing; Yu, Zhijian

doi:10.1021/acsinfecdis.3c00387

ACS Infect. Dis.

2023

DOI: 10.1021/acsinfecdis.3c00387

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Thiazolopyrimidinone Derivative H5–23 Enhances Daptomycin Activity against Linezolid-Resistant Enterococcus faecalis by Disrupting the Cell Membrane

Yanpeng Xiong,

Zhong Chen,

Bing Bai

et al.

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Cited by 3 publications

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Discovery of novel dihydropyrrolidone-thiadiazole compound crosstalk between the YycG/F two-component regulatory pathway and cell membrane homeostasis to combat methicillin-resistant Staphylococcus aureus

Xiong,

Wang,

Zheng

et al. 2024

European Journal of Medicinal Chemistry

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Discovery of novel dihydropyrrolidone-thiadiazole compound crosstalk between the YycG/F two-component regulatory pathway and cell membrane homeostasis to combat methicillin-resistant Staphylococcus aureus

Xiong,

Wang,

Zheng

et al. 2024

European Journal of Medicinal Chemistry

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2,4-Bisphenol S triggers physiological changes, oxidative stress and lipidome alterations in Gram-positive Enterococcus faecalis at environmental concentrations

Chen,

An,

et al. 2025

Environmental Pollution

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Repurposing Benzbromarone as an Antibacterial Agent against Gram-Positive Bacteria

Meng,

Wang,

Huang

et al. 2024

ACS Infect. Dis.

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The rise of antibiotic-resistant Gram-positive pathogens, particularly methicillin-resistant Staphylococcus aureus (MRSA), presents a significant challenge in clinical settings. There is a critical need for new antibacterial agents to combat these resistant strains. Our study reveals that the uricosuric drug Benzbromarone (Benz) exhibits potent antibacterial activity against Gram-positive pathogens, with minimum inhibitory concentrations (MICs) ranging from 8 to 32 μg/mL and minimum bactericidal concentrations (MBCs) ranging from 32 to 128 μg/ mL against clinical isolates of S. aureus, S. epidermidis, Enterococcus faecalis, and Streptococcus agalactiae. Furthermore, Benz significantly inhibits biofilm formation at subinhibitory concentrations and eradicates mature biofilms at higher concentrations. Benz also suppresses the hemolytic activity of S. aureus, indicating its potential to reduce virulence. Proteomic and in vitro induced resistance analyses indicate that Benz inhibits protein synthesis and turnover. Additionally, Benz induces membrane depolarization and increases membrane permeability, likely by targeting the membrane phospholipid phosphatidylethanolamine (PE). In the mouse wound infection model, Benz promotes wound healing and significantly reduces bacterial load. These findings suggest that Benz is a promising candidate for developing new antibacterial therapies against Gram-positive bacterial infections.

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Thiazolopyrimidinone Derivative H5–23 Enhances Daptomycin Activity against Linezolid-Resistant Enterococcus faecalis by Disrupting the Cell Membrane

Cited by 3 publications

References 39 publications

Discovery of novel dihydropyrrolidone-thiadiazole compound crosstalk between the YycG/F two-component regulatory pathway and cell membrane homeostasis to combat methicillin-resistant Staphylococcus aureus

Discovery of novel dihydropyrrolidone-thiadiazole compound crosstalk between the YycG/F two-component regulatory pathway and cell membrane homeostasis to combat methicillin-resistant Staphylococcus aureus

2,4-Bisphenol S triggers physiological changes, oxidative stress and lipidome alterations in Gram-positive Enterococcus faecalis at environmental concentrations

Repurposing Benzbromarone as an Antibacterial Agent against Gram-Positive Bacteria

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