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Total Synthesis and Structure–Activity Relationships Study of Odilorhabdins, a New Class of Peptides Showing Potent Antibacterial Activity

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posted on 07.08.2018, 00:00 by Matthieu Sarciaux, Lucile Pantel, Camille Midrier, Marine Serri, Cristelle Gerber, Renata Marcia de Figueiredo, Jean-Marc Campagne, Philippe Villain-Guillot, Maxime Gualtieri, Emilie Racine
The spread of antibiotic-resistant pathogens is a growing concern, and new families of antibacterials are desperately needed. Odilorhabdins are a new class of antibacterial compounds that bind to the bacterial ribosome and kill bacteria through inhibition of the translation. NOSO-95C, one of the first member of this family, was synthesized for the first time, and then a structure–activity relationships study was performed to understand which groups are important for antibacterial activity and for inhibition of the bacterial translation. Based on this study an analogue showing improved properties compared to the parent compound was identified and showed promising in vitro and in vivo efficacy against Enterobacteriaceae.