Initial efforts toward the optimization of arylomycins for antibiotic activity

T.C. Roberts, M. Schallenberger, J. Liu, P.A. Smith, F.E. Romesberg, J. Med. Chem. (2011) 54:4954-4963.
pubpic2010xxResistance to the arylomycins in several key human pathogens is due to the presence of a specific Pro residue in the target peptidase that disrupts interactions with the lipopeptide tail of the antibiotic. Here, we describe the synthesis and characterization of arylomycin derivatives with altered lipopeptide tails, including several with an increased spectrum of activity against S. aureus.