The Synthesis and Biological Evaluation of a Novel Pleuromutilin Derivative Containing a 4-Fluorophenyl Group Targeting MRSA DOI Creative Commons

Yongfei Wang,

Yi Zhao,

Haiting Wang

и другие.

Molecules, Год журнала: 2025, Номер 30(11), С. 2366 - 2366

Опубликована: Май 29, 2025

The pleuromutilin derivative, the compound PL-W, was synthesized by introducing a 4-fluorophenyl group at C21 position and selected for comprehensive antibacterial evaluation. PL-W demonstrated notable activity against methicillin-resistant Staphylococcus aureus (MRSA), with minimum inhibitory concentration (MIC) of 0.03125 µg/mL, which is significantly lower than that tiamulin (0.5 µg/mL). Crystal violet (CV) staining revealed it inhibited MRSA biofilm formation electron microscopy disrupted bacterial cell division and, possibly, synthesis essential wall proteins. In both in vivo models, exhibited excellent performance. Galleria mellonella infection model, treatment different concentrations increased survival rate from 20% to 90% reduced load. mouse model pneumonia, 10 mg/kg dose 70%, decreased load lungs, alleviated inflammatory damage. Molecular docking studies indicated had similar pose comparable binding affinity lefamulin, hydrogen bond interactions are crucial peptidyl transferase center (PTC). Moreover, no significant reduction viability HepG2 HEK293 cells, even high (≤50 Overall, shows potential as novel anti-MRSA agent owing its potent vitro activities low cytotoxicity.

Язык: Английский

Design, Synthesis and Evaluation of Novel 1,3-Benzodioxole Derivatives for Their Anti-Tumor Activity DOI
Jing Ji,

Bing-Yan Wang,

Lu Cheng

и другие.

Опубликована: Янв. 1, 2025

Язык: Английский

Процитировано

0
From Natural Products to Small Molecules: Recent Advancements in Anti-MRSA Therapeutics DOI Creative Commons
Jack W. Smith, A. LeBlanc, William M. Wuest

и другие.

ACS Medicinal Chemistry Letters, Год журнала: 2025, Номер 16(4), С. 542 - 551

Опубликована: Март 14, 2025

The urgent need for unique small molecules to treat increasing resistance in gram-positive pathogens, particularly methicillin-resistant Staphylococcus aureus, has motivated several creative research endeavors over the past decade. Recent advances have been inspired by natural products such as pleuromutilin, discovered high-throughput screens, or repurposed approved drugs like sorafenib. This microperspective spotlights bioactive compounds, ranging from molecule scaffolds, that reported recent literature, highlighting their mechanisms of action, structure-activity relationships, and future potential.

Язык: Английский

Процитировано

0
Pharmacokinetic/pharmacodynamic relationship of a novel pleuromutilin derivative p-furoylamphenmulin against Mycoplasma gallisepticum in vivo in chickens DOI Creative Commons

Xirui Xia,

Huifang Zhao, Yaxi Li

и другие.

Poultry Science, Год журнала: 2025, Номер unknown, С. 105249 - 105249

Опубликована: Май 1, 2025

Язык: Английский

Процитировано

0
The Synthesis and Biological Evaluation of a Novel Pleuromutilin Derivative Containing a 4-Fluorophenyl Group Targeting MRSA DOI Creative Commons

Yongfei Wang,

Yi Zhao,

Haiting Wang

и другие.

Molecules, Год журнала: 2025, Номер 30(11), С. 2366 - 2366

Опубликована: Май 29, 2025

The pleuromutilin derivative, the compound PL-W, was synthesized by introducing a 4-fluorophenyl group at C21 position and selected for comprehensive antibacterial evaluation. PL-W demonstrated notable activity against methicillin-resistant Staphylococcus aureus (MRSA), with minimum inhibitory concentration (MIC) of 0.03125 µg/mL, which is significantly lower than that tiamulin (0.5 µg/mL). Crystal violet (CV) staining revealed it inhibited MRSA biofilm formation electron microscopy disrupted bacterial cell division and, possibly, synthesis essential wall proteins. In both in vivo models, exhibited excellent performance. Galleria mellonella infection model, treatment different concentrations increased survival rate from 20% to 90% reduced load. mouse model pneumonia, 10 mg/kg dose 70%, decreased load lungs, alleviated inflammatory damage. Molecular docking studies indicated had similar pose comparable binding affinity lefamulin, hydrogen bond interactions are crucial peptidyl transferase center (PTC). Moreover, no significant reduction viability HepG2 HEK293 cells, even high (≤50 Overall, shows potential as novel anti-MRSA agent owing its potent vitro activities low cytotoxicity.

Язык: Английский

Процитировано

0