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 journalArticle

14 Scopus citations

Abstract

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
Volume17
Issue number5
DOIs
StatePublished - 1 Mar 2007

Keywords

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

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    Kim, I. H., Combrink, K. D., Ma, Z., Chapo, K., Yan, D., Renick, P., Morris, T. W., Pulse, M., Simecka, J. W., & Ding, C. Z. (2007). Synthesis and antibacterial evaluation of a novel series of rifabutin-like spirorifamycins. Bioorganic and Medicinal Chemistry Letters, 17(5), 1181-1184. https://doi.org/10.1016/j.bmcl.2006.12.026