15870-91-4Relevant articles and documents
Development of Amphiphilic Coumarin Derivatives as Membrane-Active Antimicrobial Agents with Potent in Vivo Efficacy against Gram-Positive Pathogenic Bacteria
Zhong, Rongcui,Li, Haizhou,Li, Hongxia,Fang, Shanfang,Liu, Jiayong,Chen, Yongzhi,Liu, Shouping,Lin, Shuimu
, p. 2864 - 2875 (2021/09/28)
Increases in drug-resistant pathogens are becoming a serious detriment to human health. To combat pathogen infections, a new series of amphiphilic coumarin derivatives were designed and synthesized as antimicrobial agents with membrane-targeting action. We herein report a lead compound, 25, that displayed potent antibacterial activity against Gram-positive bacteria, including MRSA. Compound 25 exhibited weak hemolytic activity and low toxicity to mammalian cells and can kill Gram-positive bacteria quickly (within 0.5 h) by directly disrupting the bacterial cell membranes. Additionally, compound 25 demonstrated excellent efficacy in a murine corneal infection caused by Staphylococcus aureus. These results suggest that 25 has great potential to be a potent antimicrobial agent for treating drug-resistant Gram-positive bacterial infections.
