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Lipopeptidomimetics derived from teixobactin have potent antibacterial activity against Staphylococcus aureus.

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journal contribution
posted on 2019-06-03, 14:02 authored by GC Girt, A Mahindra, ZJH Al Jabri, M De Ste Croix, MR Oggioni, AG Jamieson
A series of lipopeptidomimetics derived from teixobactin have been prepared that probe the role of residues (1-6) as a membrane anchor and the function of enduracididine. The most active compounds, with a farnesyl tail and End10 to Lys10 or Orn10 substitution have potent activity (MIC 8 μg mL-1) against S. aureus. These results pave the way for the synthesis of simple, cost-effective yet potent lipopeptidomimetic antimicrobials.

Funding

The authors would like to thank the Universities of Leicester and Glasgow, the ERDF (IRSA) and Pepceuticals Ltd for funding. We gratefully acknowledge Mick Lee (University of Leicester) for LCMS and Gerry Griffith (University of Leicester) for NMR.

History

Citation

Chemical Communications, 2018, 54 (22), pp. 2767-2770

Author affiliation

/Organisation/COLLEGE OF LIFE SCIENCES/Biological Sciences/Genetics and Genome Biology

Version

  • VoR (Version of Record)

Published in

Chemical Communications

Publisher

Royal Society of Chemistry

eissn

1364-548X

Acceptance date

2018-02-19

Copyright date

2018

Available date

2019-06-03

Publisher version

https://pubs.rsc.org/en/content/articlelanding/2018/CC/C7CC06093A#!divAbstract

Notes

Electronic supplementary information (ESI) available: Synthetic methods, LCMS, HPLC, HRMS, 1D NMR, TOCSY NMR. See DOI: 10.1039/c7cc06093a

Language

en

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