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© Research
Publication : Journal of medicinal chemistry

Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase

Team: Group: Biochemistry and chemobiology
Team: Archived: Group : Chemistry and Biocatalysis
Member: Hélène Munier-Lehmann
Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Journal of medicinal chemistry - 01 Dec 2004

Vanheusden V, Munier-Lehmann H, Froeyen M, Busson R, Rozenski J, Herdewijn P, Van Calenbergh S

Link to Pubmed [PMID] – 15566289

J. Med. Chem. 2004 Dec;47(25):6187-94

Thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for selectively blocking bacterial DNA synthesis. Hereby, we report on the discovery of a novel class of bicyclic nucleosides (10 and 11) and one dinucleoside (12), belonging to the most selective inhibitors of TMPKmt discovered so far.