Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry and Materials Science, Northwest University, Xi'an 710069, China.
Shaanxi Key Laboratory of Degradable Biomedical Materials, Shaanxi R&D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University, Xi'an 710069, China.
Molecules. 2024 Aug 21;29(16):3937. doi: 10.3390/molecules29163937.
Herein, we report a new strategy for the design of antibiotic agents based on the electrostatic interaction and hydrogen bonding, highlighting the significance of hydrogen bonding and the increased recognition sites in facilitating the interaction with bacterial cell membranes and DNA. A series of quaternary ammonium functionalized urea-based anion receptors were studied. While the monodentate mono-urea , bisurea , and trisurea failed to break through the cell membrane barrier and thus could not kill bacteria, the extended bidentate dimers - presented gradually increased membrane penetrating capabilities, DNA conformation perturbation abilities, and broad-spectrum antibacterial activities against , , , , and .
在此,我们报告了一种基于静电相互作用和氢键的新型抗生素设计策略,强调了氢键的重要性以及增加的识别位点有助于与细菌细胞膜和 DNA 相互作用。我们研究了一系列季铵官能化的基于脲的阴离子受体。虽然单齿单脲、双脲和三脲未能突破细胞膜屏障,因此无法杀死细菌,但扩展的双齿二聚体-逐渐表现出增强的膜穿透能力、DNA 构象扰动能力以及广谱抗菌活性,可对抗 、 、 、 、 和 。