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The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK)

Author
Organization
Abstract
Thymidylate kinase (TMPK) phosphorylates thymidine 5’-monophosphate (dTMP) to thymidine 5’-diphosphate (dTDP) and has been proposed as an attractive anti-tubercular target. By mimicking the structure of the substrate (dTMP), we have previously discovered different series of nucleoside analogues with Mycobacterium tuberculosis (Mt) TMPK inhibitory activities in the micromolar range. Based on recently reported potent piperidin-3-yl-thymine inhibitors of Gram-positive bacterial TMPK, we report a series of isomeric N-benzyl-substituted piperidin-4-yl-thymine analogues, some of which demonstrate very promising MtTMPK inhibitory potency. This poster will discuss the synthesis, MtTMPK inhibitory activity, as well as structural data on how these new inhibitors interact with the target enzyme.

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MLA
Song, Lijun, Martijn Risseeuw, Fabian Hulpia, et al. “The Design and Synthesis of Inhibitors of Mycobacterium Tuberculosis Thymidylate Kinase (MtTMPK).” Nucleosides, Nucleotides and Nucleic Acids, XXII Round Table, Abstracts. 2016. 180–180. Print.
APA
Song, L., Risseeuw, M., Hulpia, F., Merceron, R., Savvides, S., Munier-Lehmann, H., & Van Calenbergh, S. (2016). The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK). Nucleosides, Nucleotides and Nucleic Acids, XXII Round table, Abstracts (pp. 180–180). Presented at the 22nd International roundtable on Nucleosides, Nucleotides and Nucleic Acids.
Chicago author-date
Song, Lijun, Martijn Risseeuw, Fabian Hulpia, Romain Merceron, Savvas Savvides, Hélène Munier-Lehmann, and Serge Van Calenbergh. 2016. “The Design and Synthesis of Inhibitors of Mycobacterium Tuberculosis Thymidylate Kinase (MtTMPK).” In Nucleosides, Nucleotides and Nucleic Acids, XXII Round Table, Abstracts, 180–180.
Chicago author-date (all authors)
Song, Lijun, Martijn Risseeuw, Fabian Hulpia, Romain Merceron, Savvas Savvides, Hélène Munier-Lehmann, and Serge Van Calenbergh. 2016. “The Design and Synthesis of Inhibitors of Mycobacterium Tuberculosis Thymidylate Kinase (MtTMPK).” In Nucleosides, Nucleotides and Nucleic Acids, XXII Round Table, Abstracts, 180–180.
Vancouver
1.
Song L, Risseeuw M, Hulpia F, Merceron R, Savvides S, Munier-Lehmann H, et al. The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK). Nucleosides, Nucleotides and Nucleic Acids, XXII Round table, Abstracts. 2016. p. 180–180.
IEEE
[1]
L. Song et al., “The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK),” in Nucleosides, Nucleotides and Nucleic Acids, XXII Round table, Abstracts, Paris, France, 2016, pp. 180–180.
@inproceedings{8150287,
  abstract     = {{Thymidylate kinase (TMPK) phosphorylates thymidine 5’-monophosphate (dTMP) to thymidine 5’-diphosphate (dTDP) and has been proposed as an attractive anti-tubercular target. By mimicking the structure of the substrate (dTMP), we have previously discovered different series of nucleoside analogues with Mycobacterium tuberculosis (Mt) TMPK inhibitory activities in the micromolar range. Based on recently reported potent piperidin-3-yl-thymine inhibitors of Gram-positive bacterial TMPK, we report a series of isomeric N-benzyl-substituted piperidin-4-yl-thymine analogues, some of which demonstrate very promising MtTMPK inhibitory potency. This poster will discuss the synthesis, MtTMPK inhibitory activity, as well as structural data on how these new inhibitors interact with the target enzyme.}},
  author       = {{Song, Lijun and Risseeuw, Martijn and Hulpia, Fabian and Merceron, Romain and Savvides, Savvas and Munier-Lehmann, Hélène and Van Calenbergh, Serge}},
  booktitle    = {{Nucleosides, Nucleotides and Nucleic Acids, XXII Round table, Abstracts}},
  language     = {{eng}},
  location     = {{Paris, France}},
  pages        = {{180--180}},
  title        = {{The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK)}},
  year         = {{2016}},
}