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© Research
Publication : Bioorganic & medicinal chemistry letters

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

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Bioorganic & medicinal chemistry letters - 01 Oct 2002

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

Link to Pubmed [PMID] – 12217356

Bioorg. Med. Chem. Lett. 2002 Oct;12(19):2695-8

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.