Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

Abstract : We report the design and synthesis of a series of non-nucleoside MtbTMPK inhibitors (1-14) based on the gram-positive bacterial TMPK inhibitor hit compound 1. A practical synthesis was developed to access these analogues. Several compounds show promising MtbTMPK inhibitory potency and allow the establishment of a structure-activity relationship, which is helpful for further optimization.
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Lijun Song, Martijn D.P. Risseeuw, Matheus Froeyen, Izet Karalic, Jan Goeman, et al.. Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents. Bioorganic & medicinal chemistry, Elsevier, 2016, 24 (21), pp.5172 - 5182. ⟨10.1016/j.bmc.2016.08.041⟩. ⟨pasteur-01616045⟩

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