Synthesis and evaluation of 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 : 2002

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

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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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pasteur-00166198 , version 1 (01-08-2007)

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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, 2002, 12 (19), pp.2695-8. ⟨10.1016/S0960-894X(02)00551-6⟩. ⟨pasteur-00166198⟩

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