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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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