Synthesis and Biological Evaluation of Inhibitors of Thymidine Monophosphate Kinase from Bacillus Anthracis |
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| Authors: | Youngjoo Byun Susan R Vogel Andrew J Phipps Cecilia Carnrot Staffan Eriksson Rohit Tiwari |
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| Institution: | 1. Department of Radiology , Johns Hopkins Medical Institutions , Baltimore , Maryland , USA;2. Department of Veterinary Biosciences and Center for Microbial Interface Biology , The Ohio State University , Columbus , Ohio , USA;3. Department of Anatomy, Physiology and Biochemistry, BMC , Swedish University of Agricultural Sciences , Uppsala , Sweden;4. College of Pharmacy and Center for Microbial Interface Biology , The Ohio State University , Columbus , Ohio , USA |
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| 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. |
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| Keywords: | Bacillus anthracis thymidine monophosphate kinase (BaTMPK) 5′-Modified thymidine-based BaTMPK kinase inhibitors |
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