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

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Sarciaux M,Pantel L,Midrier C,Serri M,Gerber C,Marcia de Figueiredo R,Campagne JM,Villain-Guillot P,Gualtieri M,Racine E

doi

10.1021/acs.jmedchem.8b00790

subject

Has Abstract

pub_date

2018-09-13 00:00:00

pages

7814-7826

issue

17

eissn

0022-2623

issn

1520-4804

journal_volume

61

pub_type

杂志文章

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