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

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Abstract
Thymidylate kinase (TMPK) phosphorylates thymidine 5’-monophosphate (dTMP) and has been proposed as an attractive target for Mycobacterium tuberculosis (Mt).1 By mimicking the structure of the substrate (dTMP), we have previously discovered different series of nucleoside analogues with MtTMPK inhibitory activities in a micromole range.2 Based on recently reported potent piperidin-3-yl-thymine inhibitors of Gram-positive bacterial TMPK,3 we report a series of isomeric N-benzyl-substituted piperidin-4-yl-thymine analogues, some of which demonstrate potent Mt TMPK inhibitory activity. Towards this end a convenient and high-yield synthesis was developed to access 1-substitued thymine derivatives.

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MLA
Song, Lijun, et al. “The Design and Synthesis of Inhibitors of Mycobacterium Tuberculosis Thymidylate Kinase (MtTMPK).” Frontiers in Medicinal Chemistry, Abstracts, Scientific Conference Producers, 2015, pp. 254–254.
APA
Song, L., Risseeuw, M., Hulpia, F., Munier-Lehmann, H., & Van Calenbergh, S. (2015). The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK). In Frontiers in Medicinal Chemistry, Abstracts (pp. 254–254). Antwerp, Belgium: Scientific Conference Producers.
Chicago author-date
Song, Lijun, Martijn Risseeuw, Fabian Hulpia, Hélène Munier-Lehmann, and Serge Van Calenbergh. 2015. “The Design and Synthesis of Inhibitors of Mycobacterium Tuberculosis Thymidylate Kinase (MtTMPK).” In Frontiers in Medicinal Chemistry, Abstracts, 254–254. Scientific Conference Producers.
Chicago author-date (all authors)
Song, Lijun, Martijn Risseeuw, Fabian Hulpia, Hélène Munier-Lehmann, and Serge Van Calenbergh. 2015. “The Design and Synthesis of Inhibitors of Mycobacterium Tuberculosis Thymidylate Kinase (MtTMPK).” In Frontiers in Medicinal Chemistry, Abstracts, 254–254. Scientific Conference Producers.
Vancouver
1.
Song L, Risseeuw M, Hulpia F, Munier-Lehmann H, Van Calenbergh S. The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK). In: Frontiers in Medicinal Chemistry, Abstracts. Scientific Conference Producers; 2015. p. 254–254.
IEEE
[1]
L. Song, M. Risseeuw, F. Hulpia, H. Munier-Lehmann, and S. Van Calenbergh, “The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK),” in Frontiers in Medicinal Chemistry, Abstracts, Antwerp, Belgium, 2015, pp. 254–254.
@inproceedings{6934265,
  abstract     = {{Thymidylate kinase (TMPK) phosphorylates thymidine 5’-monophosphate (dTMP) and has been proposed as an attractive target for Mycobacterium tuberculosis (Mt).1 By mimicking the structure of the substrate (dTMP), we have previously discovered different series of nucleoside analogues with MtTMPK inhibitory activities in a micromole range.2 Based on recently reported potent piperidin-3-yl-thymine inhibitors of Gram-positive bacterial TMPK,3 we report a series of isomeric N-benzyl-substituted piperidin-4-yl-thymine analogues, some of which demonstrate potent Mt TMPK inhibitory activity. Towards this end a convenient and high-yield synthesis was developed to access 1-substitued thymine derivatives.}},
  author       = {{Song, Lijun and Risseeuw, Martijn and Hulpia, Fabian and Munier-Lehmann, Hélène and Van Calenbergh, Serge}},
  booktitle    = {{Frontiers in Medicinal Chemistry, Abstracts}},
  language     = {{eng}},
  location     = {{Antwerp, Belgium}},
  pages        = {{254--254}},
  publisher    = {{Scientific Conference Producers}},
  title        = {{The design and synthesis of inhibitors of Mycobacterium tuberculosis thymidylate kinase (MtTMPK)}},
  year         = {{2015}},
}