Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins

In Ho Kim, Keith D. Combrink, Zhenkun Ma, Katrina Chapo, Dalai Yan, Paul Renick, Timothy W. Morris, Mark Pulse, Jerry W. Simecka, Charles Z. Ding

Research output: Contribution to journalArticlepeer-review

15 Scopus citations


A novel series of spirorifamycins was synthesized and their antibacterial activity evaluated both in vitro and in vivo. This new series of rifamycins shows excellent activity against Staphylococcus aureus that is equivalent to rifabutin. However, some compounds of the series exhibit lower MICs than rifabutin against rifampin-resistant strains of S. aureus. Further, compound 2e exhibits comparable efficacy in vivo in a murine model of S. aureus septicemia model following administration by either oral or parenteral dosing routes.

Original languageEnglish
Pages (from-to)1181-1184
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number5
StatePublished - 1 Mar 2007


  • Ansamycin
  • Antibacterial
  • RNA polyerase inhibitors
  • Rifabutin
  • Rifampin-resistant
  • Rifamycin
  • Spirorifamycin
  • Staphylococcus aureus
  • Synthesis


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