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阳离子柱芳烃与外排泵抑制剂杂化化合物对革兰氏阴性菌的协同作用。

Synergistic effect of the hybrid compounds of cationic pillararene and an efflux pump inhibitor against Gram-negative bacteria.

作者信息

Liu Yisu, Wu Guangpu, Zhu Jiang, Jiang Yao, Liu Hui

机构信息

Key Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering & Pharmacy, Wuhan Institute of Technology 693 Xiongchu Avenue Wuhan 430073 P. R. China

Medical Imaging Key Laboratory of Sichuan Province, North Sichuan Medical College Nanchong 637000 Sichuan P. R. China.

出版信息

RSC Med Chem. 2025 Jun 4. doi: 10.1039/d5md00262a.

Abstract

Novel antibiofilm agents were designed by integrating cationic pillararene with an efflux pump inhibitor. The hybrid compounds were prepared and characterized using NMR and HRMS. These compounds exhibited potent activity to inhibit biofilm formation and disrupt the outer membrane in Gram-negative bacteria. In addition, the synergistic effect of the hybrid compounds was observed in combination with antibiotics, especially against . The hybridization strategy not only reduced the dosages required for the efflux pump inhibitor but also enhanced the antibacterial efficacy of antibiotics, making this a promising approach for developing antibacterial drugs.

摘要

通过将阳离子柱芳烃与外排泵抑制剂整合来设计新型抗生物膜剂。制备了这些杂化化合物,并使用核磁共振(NMR)和高分辨质谱(HRMS)对其进行了表征。这些化合物在抑制革兰氏阴性菌生物膜形成和破坏外膜方面表现出强大的活性。此外,观察到这些杂化化合物与抗生素联合使用时具有协同效应,尤其是对……。这种杂交策略不仅降低了外排泵抑制剂所需的剂量,还增强了抗生素的抗菌效果,使其成为开发抗菌药物的一种有前景的方法。

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