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

Publication: Contribution to journal › Journal article › peer-review

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
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
Publication status	Published - 2008

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

bacillus anthracis thymidine monophosphate kinase (BaTMPK)
5'-modified
thymidine-based BaTMPK kinase inhibitors

Access to Document

10.1080/15257770701845238

Cite this

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title = "Synthesis and biological evaluation of inhibitors of thymidine monophosphate kinase from Bacillus anthracis",

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.",

keywords = "bacillus anthracis thymidine monophosphate kinase (BaTMPK), 5'-modified, thymidine-based BaTMPK kinase inhibitors, bacillus anthracis thymidine monophosphate kinase (BaTMPK), 5'-modified, thymidine-based BaTMPK kinase inhibitors",

author = "Youngjoo Byun and Vogel, \{Susan R.\} and Phipps, \{Andrew J.\} and Cecilia Carnrot and Staffan Eriksson and Rohit Tiwari and Werner Tjarks",

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doi = "10.1080/15257770701845238",

language = "English",

volume = "27",

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journal = "Nucleosides, Nucleotides and Nucleic Acids",

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T1 - Synthesis and biological evaluation of inhibitors of thymidine monophosphate kinase from Bacillus anthracis

AU - Byun, Youngjoo

AU - Vogel, Susan R.

AU - Phipps, Andrew J.

AU - Carnrot, Cecilia

AU - Eriksson, Staffan

AU - Tiwari, Rohit

AU - Tjarks, Werner

PY - 2008

Y1 - 2008

N2 - 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.

AB - 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.

KW - bacillus anthracis thymidine monophosphate kinase (BaTMPK)

KW - 5'-modified

KW - thymidine-based BaTMPK kinase inhibitors

KW - bacillus anthracis thymidine monophosphate kinase (BaTMPK)

KW - 5'-modified

KW - thymidine-based BaTMPK kinase inhibitors

UR - https://res.slu.se/id/publ/20801

U2 - 10.1080/15257770701845238

DO - 10.1080/15257770701845238

M3 - Journal article

C2 - 18260009

SN - 1525-7770

VL - 27

SP - 244

EP - 260

JO - Nucleosides, Nucleotides and Nucleic Acids

JF - Nucleosides, Nucleotides and Nucleic Acids

IS - 3

ER -

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

Abstract

UN SDGs

Keywords

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