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© Institut Pasteur
Cristaux de cellulase, enzyme purifiée de Clostridium thermocellum permettant la digestion de la cellulose. Image colorisée.
Publication : Bioorganic & medicinal chemistry letters

Thymidine and thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Bioorganic & medicinal chemistry letters - 15 Sep 2003

Vanheusden V, Van Rompaey P, Munier-Lehmann H, Pochet S, Herdewijn P, Van Calenbergh S

Link to Pubmed [PMID] – 12941330

Bioorg. Med. Chem. Lett. 2003 Sep;13(18):3045-8

The affinity of a series of 2′, 3′- and 5-modified thymidine analogues for Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) was evaluated. The affinities of several non-phosphorylated analogues are in the same order of magnitude as those of their phosphorylated congeners. In view of drug delivery problems associated with phosphorylated compounds, these ‘free’ nucleosides seem more promising leads in the search of TMPKmt inhibitors as novel anti-tuberculosis agents.

http://www.ncbi.nlm.nih.gov/pubmed/12941330