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1-(1-Arylethylpiperidin-4-yl)thymine analogs as antimycobacterial TMPK inhibitors

Journal Contribution - e-publication

A series ofMycobacterium tuberculosisTMPK (MtbTMPK) inhibitors based on a reported compound3were synthesized and evaluated for their capacity to inhibitMtbTMPK catalytic activity and the growth of a virulentM. tuberculosisstrain (H37Rv). Modifications of the scaffold of3failed to afford substantial improvements inMtbTMPK inhibitory activity and antimycobacterial activity. Optimization of the substitution pattern of the D ring of3resulted in compound21jwith improvedMtbTMPK inhibitory potency (three-fold) and H37Rv growth inhibitory activity (two-fold). Moving the 3-chloro substituent of21jto thepara-position afforded isomer21h, which, despite a 10-fold increase in IC50-value, displayed promising whole cell activity (minimum inhibitory concentration (MIC) = 12.5 mu M).
Journal: Molecules: a journal of synthetic chemistry and natural product chemistry
ISSN: 1420-3049
Volume: 25
Publication year:2020
Keywords:A1 Journal article
BOF-keylabel:yes
BOF-publication weight:1
CSS-citation score:1
Authors:International
Authors from:Higher Education
Accessibility:Open