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

Veerle Vanheusden 1 Hélène Munier-Lehmann 2 Sylvie Pochet 3 Piet Herdewijn 1, 4 Serge van Calenbergh 1
1 UGENT - Ghent University [Belgium]
2 CSM - Chimie Structurale des Macromolécules
3 Chimie Organique
4 KU Leuven - Catholic University of Leuven - Katholieke Universiteit Leuven
Abstract : A number of 2'- and 3'-modified thymidine 5'-O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate kinase showed that a 2'-halogeno substituent and a 3'-azido function are the most favorable leads for further development of potent inhibitors of this enzyme.
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https://hal-pasteur.archives-ouvertes.fr/pasteur-00166198
Contributor : Sylvie Pochet <>
Submitted on : Wednesday, August 1, 2007 - 6:41:08 PM
Last modification on : Monday, March 8, 2021 - 4:12:02 PM

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Veerle Vanheusden, Hélène Munier-Lehmann, Sylvie Pochet, Piet Herdewijn, Serge van Calenbergh. Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2002, 12 (19), pp.2695-8. ⟨10.1016/S0960-894X(02)00551-6⟩. ⟨pasteur-00166198⟩

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