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

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Song, Lijun | Risseeuw, Martijn D.P. | Froeyen, Matheus | Karalic, Izet | Goeman, Jan | Cappoen, Davie | van Der Eycken, Johan | Cos, Paul | Munier-Lehmann, Hélène | van Calenbergh, Serge | Risseeuw, Martijn, D P | Froeyen, Mathy

Edité par CCSD ; Elsevier -

International audience. 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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