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

Lijun Song 1 Martijn D.P. Risseeuw 1 Matheus Froeyen 2 Izet Karalic 1 Jan Goeman 1 Davie Cappoen 3 Johan van der Eycken 1 Paul Cos 3 Hélène Munier-Lehmann 4 Serge van Calenbergh 1, * Martijn Risseeuw Mathy Froeyen 5
* Corresponding author
1 UGENT - Ghent University [Belgium]
2 Rega Institute for Medical Research [Leuven, België]
3 UA - University of Antwerp
4 Chimie et Biocatalyse
5 KU Leuven - Catholic University of Leuven - Katholieke Universiteit Leuven
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.
Keywords : Inhibitors Mycobacterium tuberculosis Thymidine monophosphate kinase Thymine derivatives XDR-TB extensively drug-resistant tuberculosis
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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 and Medicinal Chemistry, Elsevier, 2016, 24 (21), pp.5172 - 5182. ⟨10.1016/j.bmc.2016.08.041⟩. ⟨pasteur-01616045⟩

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