Antibiotic repurposing: bis-catechol- and mixed ligand (bis-catechol-mono-hydroxamate)-teicoplanin conjugates are active against multidrug resistant Acinetobacter baumannii.,The Journal of Antibiotics

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Antibiotic repurposing: bis-catechol- and mixed ligand (bis-catechol-mono-hydroxamate)-teicoplanin conjugates are active against multidrug resistant Acinetobacter baumannii.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2019-12-13 , DOI: 10.1038/s41429-019-0268-7
Manuka Ghosh ₁ , Patricia A Miller _{1,

2} , Marvin J Miller _{1,

2}

Affiliation

Antibiotics that are normally used to treat infections caused by Gram-positive bacteria might be made effective against Gram-negative bacterial infections, if they can circumvent permeability barriers and antibiotic deactivation processes associated with Gram-negative bacteria. Herein we report syntheses of bis-catechol-teicoplanin and mixed ligand catechol-hydroxamate-teicoplanin conjugates. Antibacterial activity assays revealed that conjugation of teicoplanin, which is only known to be active against Gram-positive bacteria, to the siderophore mimics induced potent activity against multidrug resistant strains of select Gram-negative bacteria (Acinetobacter baumannii) while retaining moderate activity against Gram-positive bacteria (Staphylococcus aureus).

中文翻译：

抗生素再利用：双-邻苯二酚和混合配体（双-邻苯二酚-单异羟肟酸酯）-替考拉宁偶联物对多重耐药的鲍曼不动杆菌具有活性。

如果通常用于治疗革兰氏阳性细菌感染的抗生素可以规避与革兰氏阴性细菌有关的渗透性障碍和抗生素失活过程，那么它们可以有效抵抗革兰氏阴性细菌感染。在这里，我们报告双邻苯二酚-替考拉宁和混合配体儿茶酚-异羟肟酸酯-替考拉宁缀合物的合成。抗菌活性分析表明，仅已知对革兰氏阳性细菌有活性的替考拉宁与铁载体模拟物对选定的革兰氏阴性细菌（鲍曼不动杆菌）的多药耐药菌株诱导了有效的活性，同时保持了对革兰氏阴性细菌的中等活性。阳性细菌（金黄色葡萄球菌）。

更新日期：2019-12-13

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