Synthetic studies on the reverse antibiotic natural products, the nybomycins

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Title: Synthetic studies on the reverse antibiotic natural products, the nybomycins
Authors: Bardell-Cox, O
White, AJP
Aragón, L
Fuchter, M
Item Type: Journal Article
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.
Issue Date: 24-May-2019
Date of Acceptance: 22-May-2019
ISSN: 2040-2503
Publisher: Royal Society of Chemistry (RSC)
Journal / Book Title: MedChemComm
Copyright Statement: © 2019 The Royal Society of Chemistry.
Sponsor/Funder: Engineering & Physical Science Research Council (EPSRC)
Funder's Grant Number: EP/R00188X/1
Keywords: 0304 Medicinal and Biomolecular Chemistry
0305 Organic Chemistry
1115 Pharmacology and Pharmaceutical Sciences
Publication Status: Published online
Embargo Date: 2020-05-22
Online Publication Date: 2019-05-24
Appears in Collections:Chemistry

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