The kalimantacins are a family of hybrid polyketide-nonribosomal peptide derived natural products that display potent and selective antibiotic activity against multi-drug resistant strains of Staphylococcus aureus. Herein, we report the first total synthesis of kalimantacin A, in which three fragments are prepared and then united via Sonogashira and amide couplings. The enantioselective synthetic approach is convergent, unlocking routes to further kalimantacins and analogues for SAR studies and clinical evaluation.
- Bristol BioDesign Institute
- BCS and TECS CDTs