Synthetic studies on the reverse antibiotic natural products, the nybomycins
File(s)Bardell_Cox_etal_final_v1.pdf (586.81 KB)
Accepted version
Author(s)
Bardell-Cox, Oliver
White, Andrew JP
Aragón, Luis
Fuchter, Matthew
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.
Date Issued
2019-05-24
Date Acceptance
2019-05-22
Citation
MedChemComm, 2019, 10 (8), pp.1438-1444
ISSN
2040-2503
Publisher
Royal Society of Chemistry (RSC)
Start Page
1438
End Page
1444
Journal / Book Title
MedChemComm
Volume
10
Issue
8
Copyright Statement
© 2019 The Royal Society of Chemistry.
Sponsor
Engineering & Physical Science Research Council (EPSRC)
Identifier
https://pubs.rsc.org/en/content/articlelanding/2019/MD/C9MD00207C#!divAbstract
Grant Number
EP/R00188X/1
Subjects
Science & Technology
Life Sciences & Biomedicine
Biochemistry & Molecular Biology
Chemistry, Medicinal
Pharmacology & Pharmacy
TOPOISOMERASE-IV
STEREOSELECTIVE-SYNTHESIS
DNA GYRASE
METAL-ION
CHROMATOGRAPHY
MECHANISM
POTENT
RULES
0304 Medicinal and Biomolecular Chemistry
0305 Organic Chemistry
1115 Pharmacology and Pharmaceutical Sciences
Publication Status
Published
Date Publish Online
2019-05-24