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

Nucleosides Nucleotides Nucleic Acids. 2008 Mar;27(3):244-60. doi: 10.1080/15257770701845238.

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Bacillus anthracis / drug effects*
  • Bacillus anthracis / enzymology*
  • Bacillus anthracis / growth & development
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Nucleoside-Phosphate Kinase / antagonists & inhibitors*
  • Thymidine / analogs & derivatives*
  • Thymidine / pharmacology

Substances

  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Nucleoside-Phosphate Kinase
  • dTMP kinase
  • Thymidine