Synthesis and antimicrobial activity against Pseudomonas aeruginosa of macrocyclic β-hairpin peptidomimetic antibiotics containing N-methylated amino acids

Vetterli, Stefan U; Moehle, Kerstin; Robinson, John A

doi:10.1016/j.bmc.2016.05.027

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Vetterli, S. U., Moehle, K., & Robinson, J. A. (2016). Synthesis and antimicrobial activity against Pseudomonas aeruginosa of macrocyclic β-hairpin peptidomimetic antibiotics containing N-methylated amino acids. Bioorganic & Medicinal Chemistry, 24(24), 6332–6339. https://doi.org/10.1016/j.bmc.2016.05.027

Abstract

Antimicrobial resistance among Gram-negative bacteria is a growing problem, fueled by the paucity of new antibiotics that target these microorganisms. One novel family of macrocyclic β-hairpin-shaped peptidomimetics was recently shown to act specifically against Pseudomonas spp. by a novel mechanism of action, targeting the outer membrane protein LptD, which mediates lipopolysaccharide transport to the cell surface during outer membrane biogenesis. Here we explore the mode of binding of one of these β-hairpin peptidomimetics to LptD i