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

V Vanheusden, H Munier-Lehmann, S Pochet…

Index: Vanheusden, Veerle; Munier-Lehmann, Helene; Pochet, Sylvie; Herdewijn, Piet; Van Calenbergh, Serge Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 19 p. 2695 - 2698

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Citation Number: 53

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.