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A series of Mycobacterium tuberculosis TMPK ( Mtb TMPK) inhibitors based on a reported compound 3 were synthesized and evaluated for their capacity to inhibit Mtb TMPK catalytic activity and the growth of a virulent M. tuberculosis strain (H37Rv). Modifications of the scaffold of 3 failed to afford substantial improvements in Mtb TMPK inhibitory activity and antimycobacterial activity. Optimization of the substitution pattern of the D ring of 3 resulted in compound 21j with improved Mtb TMPK inhibitory potency (three-fold) and H37Rv growth inhibitory activity (two-fold). Moving the 3-chloro substituent of 21j to the para -position afforded isomer 21h , which, despite a 10-fold increase in IC 50 -value, displayed promising whole cell activity (minimum inhibitory concentration (MIC) = 12.5 μM).

1-(1-Arylethylpiperidin-4-yl)thymine Analogs as Antimycobacterial TMPK Inhibitors