posted on 2019-06-03, 14:02authored byGC 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