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 language | English (US) |
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Pages (from-to) | 244-260 |
Number of pages | 17 |
Journal | Nucleosides, Nucleotides and Nucleic Acids |
Volume | 27 |
Issue number | 3 |
DOIs | |
State | Published - Mar 2008 |
Keywords
- 5′-Modified thymidine-based BaTMPK kinase inhibitors
- Bacillus anthracis thymidine monophosphate kinase (BaTMPK)
ASJC Scopus subject areas
- Genetics
- Biochemistry