jm8b00790_si_002.csv (6.23 kB)
Total Synthesis and Structure–Activity Relationships Study of Odilorhabdins, a New Class of Peptides Showing Potent Antibacterial Activity
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posted on 2018-08-07, 00:00 authored by Matthieu Sarciaux, Lucile Pantel, Camille Midrier, Marine Serri, Cristelle Gerber, Renata Marcia de Figueiredo, Jean-Marc Campagne, Philippe Villain-Guillot, Maxime Gualtieri, Emilie RacineThe 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.