The impact of backbone N-methylation on the structure-activity relationship of Leu(10)-teixobactin
AuthorVelkov, T; Swarbrick, JD; Hussein, MH; Schneider-Futschik, EK; Hoyer, D; Li, J; Karas, JA
Source TitleJournal of Peptide Science
University of Melbourne Author/sHoyer, Daniel; Velkov, Tony; Hussein, Maytham; Schneider-Futschik, Elena; Karas, John; Swarbrick, James
AffiliationBiochemistry and Molecular Biology
School of Chemistry
Pharmacology and Therapeutics
Document TypeJournal Article
CitationsVelkov, T., Swarbrick, J. D., Hussein, M. H., Schneider-Futschik, E. K., Hoyer, D., Li, J. & Karas, J. A. (2019). The impact of backbone N-methylation on the structure-activity relationship of Leu(10)-teixobactin. JOURNAL OF PEPTIDE SCIENCE, 25 (9), https://doi.org/10.1002/psc.3206.
Access StatusThis item is currently not available from this repository
NHMRC Grant codeNHMRC/1128891
Antimicrobial resistance is a serious threat to global human health; therefore, new anti-infective therapeutics are required. The cyclic depsi-peptide teixobactin exhibits potent antimicrobial activity against several Gram-positive pathogens. To study the natural product's mechanism of action and improve its pharmacological properties, efficient chemical methods for preparing teixobactin analogues are required to expedite structure-activity relationship studies. Described herein is a synthetic route that enables rapid access to analogues. Furthermore, our new N-methylated analogues highlight that hydrogen bonding along the N-terminal tail is likely to be important for antimicrobial activity.
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