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

doi:10.1080/15257770701845238

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

School of Medicine

Research output: Contribution to journal › Article

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)
Pages (from-to)	244-260
Number of pages	17
Journal	Nucleosides, Nucleotides and Nucleic Acids
Volume	27
Issue number	3
DOIs	https://doi.org/10.1080/15257770701845238
State	Published - Mar 2008

Keywords

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

ASJC Scopus subject areas

Genetics
Biochemistry

Access to Document

10.1080/15257770701845238

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Byun, Y., Vogel, S. R., Phipps, A. J., Carnrot, C., Eriksson, S., Tiwari, R., & Tjarks, W. (2008). Synthesis and biological evaluation of inhibitors of thymidine monophosphate kinase from Bacillus anthracis. Nucleosides, Nucleotides and Nucleic Acids, 27(3), 244-260. https://doi.org/10.1080/15257770701845238

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