Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. - Archive ouverte HAL Access content directly
Journal Articles Bioorganic and Medicinal Chemistry Letters Year : 2003

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

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Abstract

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.

Dates and versions

pasteur-00166206 , version 1 (01-08-2007)

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Veerle Vanheusden, Philippe van Rompaey, Hélène Munier-Lehmann, Sylvie Pochet, Piet Herdewijn, et al.. Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.. Bioorganic and Medicinal Chemistry Letters, 2003, 13 (18), pp.3045-8. ⟨10.1016/S0960-894X(03)00643-7⟩. ⟨pasteur-00166206⟩

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