Please use this identifier to cite or link to this item: http://hdl.handle.net/2067/46897
Title: Antibacterial alkylguanidino ureas: Molecular simplification approach, searching for membrane-based MoA
Authors: D'Agostino, Ilaria
Ardino, Claudia
Poli, Giulio
Sannio, Filomena
Lucidi, Massimiliano
Poggialini, Federica
Visaggio, Daniela
Rango, Enrico
Filippi, Silvia
Petricci, Elena
Visca, Paolo
Lorenzo Botta 
Docquier, Jean-Denis
Dreassi, Elena
Journal: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 
Issue Date: 2022
Abstract: 
The ever-faster rise of antimicrobial resistance (AMR) represents a major global Public Health challenge. New chemical entities with innovative Modes of Action (MoAs) are thus desirable. We recently reported the development of a novel class of broad-spectrum bactericidal agents, the AlkylGuanidino Ureas (AGU). Due to their polycationic structure, they likely target bacterial membranes. In order to better understand their MoA, we synthesized a library of AGU derivatives by structural simplification of selected hit compounds and developed specific assays based on membrane models by means of both analytical and computational techniques. Cell-based assays provided experimental evidence that AGUs disrupt bacterial membranes without showing hemolytic behavior. Hence, we herein report a thorough chemical and biological characterization of a new series of AGUs obtained through molecular simplification, allowing the rational design of potent antibacterial compounds active on antibiotic-resistant strains.
URI: http://hdl.handle.net/2067/46897
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2022.114158
Rights: Attribution-NonCommercial-NoDerivatives 4.0 International
Appears in Collections:A1. Articolo in rivista

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