Identification of potent and broad-spectrum antibiotics from SAR studies of a synthetic vancomycin analogue.
Dimeric vancomycin analogues based on a lead compound identified from a library of synthetic analogues of vancomycin have up to 60-fold greater activity than vancomycin against vancomycin-resistant Enterococcus faecium (VRE, VanA phenotype). Simplified analogues have also been prepared and found to maintain activity against VRE and have broad-spectrum antibiotic activity.
Center for New Directions in Organic Synthesis, Department of Chemistry, University of California, Berkeley 94720, USA.
Kateri A
KA
Ahrendt
Jacob A
JA
Olsen
Masahiro
M
Wakao
Joaquim
J
Trias
Jonathan A
JA
Ellman
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques; D024881:Drug Resistance, Bacterial; D016984:Enterococcus faecium / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D014640:Vancomycin