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Strong Antibacterial Properties of Anion Transporters: A Result of Depolarization and Weakening of the Bacterial Membrane
journal contribution
posted on 2015-03-12, 00:00 authored by Claude
R. Elie, Guillaume David, Andreea R. SchmitzerThe development of low molecular
weight anionophores is an emerging
topic in chemistry, as the need for these compounds increases with
the continuous discovery of pathologies involving anomalies in anion
transport processes. Development of new concepts to initiate anion
imbalance in living cells while fighting multidrug-resistant bacteria
is a paramount topic. In this study, three series of compounds including N,N′-diphenylethynylbenzyl benzimidazolium
salts (1 and 2), 1,1′-(pyridine-2,6-diyl)bis(3-(4-(phenylethynyl)benzyl)-1H-benzo[d]imidazol-3-ium) salts (3–5), and 1,1′-(pyridine-2,6-diylbis(methylene))bis(3-(4-(phenyl
ethynyl)benzyl)-1H-benzo[d]imidazol-3-ium)
salts (6–8) displaying high antimicrobial
activity and low toxicity against human cells were designed, synthesized,
and studied. The most potent compound displayed micromolar minimal
inhibitory concentrations in different Gram-negative and Gram-positive
bacteria, while its hemolytic activity remained around 10% or less,
even after a prolonged period of exposure. The mechanism of action
of these benzimidazolium salts on bacterial membrane was assessed
by bioanalytical techniques including assays in model membrane liposomes,
membrane depolarization studies, and scanning electron microscopy
(SEM) in living bacteria.
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bioanalytical techniquesAnion Transporterstopicscanning electron microscopycompounds increasesmembrane depolarization studiesBacterial MembraneThe developmentSEMbenzimidazolium saltsweight anionophorespyridineanion imbalanceanion transport processesStrong Antibacterial Propertiesmodel membrane liposomesantimicrobial activity
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