Synthesis and antimicrobial evaluation of novel platensimycin analogues

Since the isolation of the natural products platensimycin and platencin as new antibiotic lead structures, several total syntheses as well as syntheses of derivatives have been developed. Most of these approaches are very laborious and the target molecules are often produced in only poor overall yields. The following approach describes the synthesis of rather simple platensimycin analogues focussing on some structure elements that have previously been identified as being essential for binding to the Fab F enzyme in fatty acid biosynthesis. Two of the new analogues show significant antimicrobial activities.