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Cationic Au(I) complexes with aryl-benzothiazoles and their antibacterial activity
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2018-05-11 , DOI: 10.1016/j.jinorgbio.2018.05.003
Jenny Stenger-Smith , Indranil Chakraborty , Pradip K. Mascharak

Two cationic Au(I) complexes derived from aryl-benzothiazoles, namely [(PPh3)Au(pbt)](OTf) (1) and [(PPh3)Au(qbt)](OTf) (2) (where pbt = 2‑(pyridyl)benzothiazole and qbt = (quinolyl)benzothiazole, and OTf = trifluoromethanesulfonate anion), have been synthesized and structurally characterized by X-ray crystallography. Both complexes exhibit strong antibacterial effects against Gram-negative bacteria such as Acinetobacter baumannii and Pseudomonas Aeruginosa. Results of examination of the reactions of 1 and 2 indicate that these cationic Au(I) complexes rapidly cross the bacterial membrane and exert drug action by disrupting cellular function(s) through binding of cytosolic thiol-containing peptides (such as glutathione) and proteins to the highly reactive (PPh3)Au+ intermediate formed upon in situ dissociation of pbt or qbt.



中文翻译:

芳基-苯并噻唑的阳离子Au(I)配合物及其抗菌活性

衍生自芳基-苯并噻唑的两种阳离子Au(I)络合物,即[(PPh 3)Au(pbt)](OTf)(1)和[(PPh 3)Au(qbt)](OTf)(2)(其中pbt = 2-(吡啶基)苯并噻唑和QBT =(喹啉基)苯并噻唑,和光学传递函数-  =三氟甲磺酸盐阴离子),已经合成和通过X射线晶体结构表征。两种复合物对革兰氏阴性细菌如鲍曼不动杆菌铜绿假单胞菌均显示出强大的抗菌作用。检查12的反应结果表明这些阳离子Au(I)配合物可快速穿过细菌膜并通过破坏细胞功能来发挥药物作用,这种作用是通过将含胞硫醇的肽(例如谷胱甘肽)和蛋白质与高反应性(PPh 3)Au +结合而破坏的在pbt或qbt原位解离时形成的中间体。

更新日期:2018-05-11
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