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© Research
Publication : Journal of enzyme inhibition and medicinal chemistry

1-(Piperidin-3-yl)thymine amides as inhibitors of M. tuberculosis thymidylate kinase.

Team: UMR3523 – Chemistry for Life Sciences (Chem4Life)
Team: Group: Biochemistry and chemobiology
Member: Hélène Munier-Lehmann
Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Journal of enzyme inhibition and medicinal chemistry - 01 Dec 2019

Jian Y, Risseeuw MDP, Froeyen M, Song L, Cappoen D, Cos P, Munier-Lehmann H, van Calenbergh S,

Link to Pubmed [PMID] – 31822127

Link to DOI – 10.1080/14756366.2019.1662790

J Enzyme Inhib Med Chem 2019 Dec; 34(1): 1730-1739

A series of readily accessible 1-(piperidin-3-yl)thymine amides was designed, synthesised and evaluated as Mycobacterium tuberculosis TMPK (MtbTMPK) inhibitors. In line with the modelling results, most inhibitors showed reasonable MtbTMPK inhibitory activity. Compounds 4b and 4i were slightly more potent than the parent compound 3. Moreover, contrary to the latter, amide analogue 4g was active against the avirulent M. tuberculosis H37Ra strain (MIC50=35 µM). This finding opens avenues for future modifications.