New Ianthelliformisamine Derivatives as Antibiotic Enhancers against Resistant Gram-Negative Bacteria

被引：48
作者：
Pieri, Cyril [1 ]
Borselli, Diane [2 ]
Di Giorgio, Carole [3 ]
De Meo, Michel [3 ]
Bolla, Jean-Michel [2 ]
Vidal, Nicolas [4 ]
Combes, Sebastien [1 ]
Brunel, Jean Michel [1 ]
机构：
[1] Aix Marseille Univ, CRCM, Inst Paoli Calmettes, CNRS,Inserm,UMR7258,UM 105,U1068, F-13009 Marseille, France
[2] Aix Marseille Univ, Fac Med, IRBA, TMCD2,UMR MD1, F-13385 Marseille, France
[3] Aix Marseille Univ, CNRS, UMR 7263, IRD 237, F-13385 Marseille 05, France
[4] Aix Marseille Univ, UPCAM ISm2, Case 342, F-13397 Marseille 13, France
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 57卷 / 10期
关键词：
OUTER-MEMBRANE; PSEUDOMONAS-AERUGINOSA; PERMEABILITY BARRIER; COLISTIN; EFFLUX; AGENTS;
D O I：
10.1021/jm500194e
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series consisting of ianthelliformisamimes A, B, and C as well as its synthetic analogues was prepared in high chemical yield, from 27 to 91%, using peptide coupling as the key step, and the compounds were evaluated for their in vitro antibiotic enhancer properties against resistant Gram-negative bacteria and clinical isolates. The mechanism of action of one of these derivatives against Pseudomonas aeruginosa when combined with doxycycline was precisely evaluated utilizing bioluminescence to measure ATP efflux and fluorescence to evaluate membrane depolarization.
引用
收藏
页码：4263 / 4272
页数：10
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