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© Research
Publication : Molecules (Basel, Switzerland)

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

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Molecules (Basel, Switzerland) - 17 Jun 2020

Jian Y, Hulpia F, D P Risseeuw M, Forbes HE, Caljon G, Munier-Lehmann H, I M Boshoff H, Van Calenbergh S,

Link to Pubmed [PMID] – 32560578

Link to DOI [DOI] – E280510.3390/molecules25122805

Molecules 2020 Jun; 25(12):

A series of Mycobacterium tuberculosis TMPK (MtbTMPK) inhibitors based on a reported compound 3 were synthesized and evaluated for their capacity to inhibit MtbTMPK catalytic activity and the growth of a virulent M. tuberculosis strain (H37Rv). Modifications of the scaffold of 3 failed to afford substantial improvements in MtbTMPK inhibitory activity and antimycobacterial activity. Optimization of the substitution pattern of the D ring of 3 resulted in compound 21j with improved MtbTMPK 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 IC50-value, displayed promising whole cell activity (minimum inhibitory concentration (MIC) = 12.5 μM).

https://pubmed.ncbi.nlm.nih.gov/32560578