Synthesis and biological evaluation of inhibitors of thymidine monophosphate kinase from Bacillus anthracis

Youngjoo Byun, Susan R. Vogel, Andrew J. Phipps, Cecilia Carnrot, Staffan Eriksson, Rohit Tiwari, Werner Tjarks

Research output: Contribution to journalArticle

Abstract

Nineteen lipophilic thymidine phosphate-mimicking compounds were designed and synthesized as potential inhibitors of thymidine monophosphate kinase of Bacillus anthracis, a Gram-positive bacterium that causes anthrax. These thymidine analogues were substituted at the 5′-postion with sulfonamide-, amide-, (thio)urea-, or triazole groups, which served as lipophilic surrogates for phosphate. Three of the tested compounds produced inhibition of B. anthracis Sterne growth and/or thymidine monophosphate activity. Additional studies will be necessary to elucidate the potential of this type of B. anthracis thymidine monophosphate inhibitors as novel antibiotics in the treatment of anthrax.

Original languageEnglish (US)
Pages (from-to)244-260
Number of pages17
JournalNucleosides, Nucleotides and Nucleic Acids
Volume27
Issue number3
DOIs
StatePublished - Mar 2008

Keywords

  • 5′-Modified thymidine-based BaTMPK kinase inhibitors
  • Bacillus anthracis thymidine monophosphate kinase (BaTMPK)

ASJC Scopus subject areas

  • Genetics
  • Biochemistry

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