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Issue 8, 2019
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Synthetic studies on the reverse antibiotic natural products, the nybomycins

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Abstract

Antimicrobial resistance (AMR) is a serious issue that could have severe consequences if steps are not taken. The nybomycin natural products have the potential to extend the clinical efficacy of the marketed fluoroquinolone class of antibiotics through a ‘reverse antibiotic’ approach. However, only very limited structure–activity relationships are known for these fascinating compounds, in part due to challenges with their synthesis. Here we report a new scalable and robust synthetic route to the nybomycin natural products to aid in the development of this series. Through this synthesis, we report the antibiotic activity of novel analogues of this family confirming the selectivity for fluoroquinolone resistant bacteria and potential future opportunities for further optimisation.

Graphical abstract: Synthetic studies on the reverse antibiotic natural products, the nybomycins

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Supplementary files

Article information


Submitted
07 Apr 2019
Accepted
22 May 2019
First published
24 May 2019

Med. Chem. Commun., 2019,10, 1438-1444
Article type
Research Article

Synthetic studies on the reverse antibiotic natural products, the nybomycins

O. A. Bardell-Cox, A. J. P. White, L. Aragón and M. J. Fuchter, Med. Chem. Commun., 2019, 10, 1438
DOI: 10.1039/C9MD00207C

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