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人工晶体学报 ›› 2023, Vol. 52 ›› Issue (10): 1842-1849.

• 研究论文 • 上一篇    下一篇

一种含吗啉修饰的多吡啶钯(Ⅱ)配合物的合成、表征与抗金黄色葡萄球菌作用研究

王润宾, 韩天植, 李知敏, 尧智玲, 廖向文, 王金涛   

  1. 江西科技师范大学药学院,南昌 330013
  • 收稿日期:2023-03-29 发布日期:2023-10-18
  • 通信作者: 廖向文,博士,副教授。E-mail:liao492008522@163.com。王金涛,博士,副教授。E-mail:jintaochem@163.com。
  • 作者简介:王润宾(1995—),男,江西省人,硕士研究生。E-mail:1176548529@qq.com
  • 基金资助:
    国家自然科学基金(22067007,22067006);江西科技师范大学大学生创新训练计划(20211504111)

Synthesis of Polypyridyl Palladium (Ⅱ) Complexes Modified with Morpholine Group and Its Antibacterial Activity Anti-Staphylococcus Aureus

WANG Runbin, HAN Tianzhi, LI Zhimin, YAO Zhiling, LIAO Xiangwen, WANG Jintao   

  1. School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, China
  • Received:2023-03-29 Published:2023-10-18

摘要: 由4′-[4-(4-吗啉基丁氧基)苯基]-2,2′∶6′,2″-三联吡啶合成了一种含吗啉修饰的三联吡啶钯配合物(Pd1),并通过核磁氢谱、元素分析和X射线单晶衍射对其结构进行表征。Pd1对金黄色葡萄球菌(S. aureus)表现出良好的抗菌活性(MIC=62.48 μg/mL, MIC为最小抑菌浓度)。通过耐药实验发现金黄色葡萄球菌对Pd1不易产生耐药性,筛选发现Pd1与盐酸克林霉素联合作用时,可以增强金黄色葡萄球菌对盐酸克林霉素的敏感性。机制研究发现Pd1对与产生耐药性有关的生物膜有明显的抑制作用。此外,Pd1对金黄色葡萄球菌产生的毒素活性具有明显的抑制作用。

关键词: 金属配合物, 多吡啶钯配合物, 吗啉, 晶体结构, 抗金黄色葡萄球菌, 联合作用

Abstract: One Polypyridyl Pd(Ⅱ) complex (Pd1) containing modified morpholine group was synthesized from 4’-[4-(4-morpholinobutyloxy) phenyl]-2,2’∶6’,2’-tripyridine and characterized by 1H NMR, element analysis and single crystal X-ray diffraction. The antibacterial activity of Pd1 was investigated against S. aureus with the MIC (minimum inhibition concentration) value of 62.48 μg/mL and the effect of Pd1 complex on S. aureus growth was investigated by growth curves. Bacteria resistance development assay indicate that the S. aureus cannot easily develop drug-resistance to Pd1. In addition, Pd1 complex can strengthen the susceptibility of S. aureus to clidamycin hydrochloride when it is combined with clidamycin hydrochloride. Meanwhile, Pd1 has a significant inhibitory effect on biofilms related to drug resistance, and show obviously inhibitory activity against the toxins from S. aureus.

Key words: metal complex, polypyridine palladium complex, morpholine, crystal structure, anti-Staphylococcus aureus, antibiotic combination

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