Development of Amphiphilic Coumarin Derivatives as Membrane-Active Antimicrobial Agents with Potent In Vivo Efficacy against Gram-Positive Pathogenic Bacteria,ACS Infectious Diseases

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Development of Amphiphilic Coumarin Derivatives as Membrane-Active Antimicrobial Agents with Potent In Vivo Efficacy against Gram-Positive Pathogenic Bacteria
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2021-09-10 , DOI: 10.1021/acsinfecdis.1c00246
Rongcui Zhong ₁ , Haizhou Li ₁ , Hongxia Li ₁ , Shanfang Fang ₁ , Jiayong Liu ₁ , Yongzhi Chen ₁ , Shouping Liu ₁ , Shuimu Lin ₁

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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.

中文翻译：

开发作为膜活性抗菌剂的两亲性香豆素衍生物，对革兰氏阳性病原菌具有强大的体内功效

耐药病原体的增加正在严重危害人类健康。为了对抗病原体感染，设计并合成了一系列新的两亲性香豆素衍生物作为具有膜靶向作用的抗菌剂。我们在此报告了一种先导化合物25，它对革兰氏阳性菌（包括 MRSA）显示出有效的抗菌活性。化合物25对哺乳动物细胞表现出弱溶血活性和低毒性，可以通过直接破坏细菌细胞膜快速（0.5小时内）杀死革兰氏阳性菌。此外，化合物25在金黄色葡萄球菌引起的鼠角膜感染中表现出优异的疗效。这些结果表明25 具有成为治疗耐药革兰氏阳性细菌感染的有效抗菌剂的巨大潜力。

更新日期：2021-10-08

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