Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents
Song, Lijun × Risseeuw, Martijn D P Froeyen, Mathy Karalic, Izet Goeman, Jan Cappoen, Davie Van der Eycken, J Cos, Paul Munier-Lehmann, Hélène Van Calenbergh, Serge #
Bioorganic & Medicinal Chemistry vol:24 issue:21
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.