当前位置: X-MOL 学术ChemMedChem › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Auranofin and its Analogues Show Potent Antimicrobial Activity against Multidrug‐Resistant Pathogens: Structure–Activity Relationships
ChemMedChem ( IF 3.4 ) Pub Date : 2018-11-05 , DOI: 10.1002/cmdc.201800498
Tiziano Marzo 1, 2 , Damiano Cirri 1 , Simona Pollini 3, 4 , Marco Prato 3 , Stefania Fallani 5 , Maria Iris Cassetta 5 , Andrea Novelli 5 , Gian Maria Rossolini 3, 4 , Luigi Messori 1
Affiliation  

Due to the so‐called “antibiotic resistance crisis” new antibacterial agents are urgently sought to treat multidrug‐resistant pathogens. A group of gold‐ or silver‐based complexes, of general formula [M(PEt3)X] (with M=Au or Ag, and X=Cl, Br or I), alongside with three complexes bearing a positive or negative charge—[Au(PEt3)2]Cl, K[Au(CN)2] and [Ag(PEt3)2]NO3—were prepared and comparatively tested with auranofin on a representative panel of pathogens including Gram‐positive, Gram‐negative and Candida strains. Interestingly, all the gold and silver complexes tested were active on Gram‐positive strains, with the gold complexes having greater efficacy. The effects of the gold compounds were potentiated to a larger extent than silver compounds when tested in combination with a permeabilizing agent. A number of relevant structure–activity relationships emerged from the comparative analysis of the observed antibacterial profiles, shedding new light on the underlying molecular mechanisms of the action of these compounds.

中文翻译:

金诺芬及其类似物显示出对多药耐药病原体的有效抗菌活性:结构与活性之间的关系

由于所谓的“抗生素耐药性危机”,迫切需要寻找新的抗菌剂来治疗具有多重耐药性的病原体。一组通式为[M(PEt 3)X]的金或银基络合物(M = Au或Ag,X = Cl,Br或I),以及三个带有正电荷或负电荷的络合物- [AU(PET 32 ]氯,K [AU(CN)2 ]和[Ag(上PET 32 ] NO 3 -were制备并比较与金诺芬病原体包括革兰氏阳性,革兰氏一个代表面板上测试阴性和念珠菌株。有趣的是,所有测试的金和银配合物都对革兰氏阳性菌株具有活性,而金配合物的功效更高。当与通透剂结合测试时,金化合物的作用比银化合物具有更大的增强作用。通过对观察到的抗菌谱进行比较分析,发现了许多相关的结构-活性关系,为这些化合物作用的潜在分子机理提供了新的思路。
更新日期:2018-11-05
down
wechat
bug