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© Institut Pasteur
Cristaux de cellulase, enzyme purifiée de Clostridium thermocellum permettant la digestion de la cellulose. Image colorisée.
Publication : Bioorganic & medicinal chemistry

Synthesis and evaluation of 5′-modified thymidines and 5-hydroxymethyl-2′-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Bioorganic & medicinal chemistry - 05 Nov 2012

Toti KS, Verbeke F, Risseeuw MD, Frecer V, Munier-Lehmann H, Van Calenbergh S

Link to Pubmed [PMID] – 23199481

Bioorg. Med. Chem. 2013 Jan;21(1):257-68

We report the synthesis of 5′-modified thymidines (16, 18, 21, 23) and 5,5′-bis-substituted 2′-deoxyuridine analogues (30, 47) as inhibitors of thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt). These analogues were evaluated for their capacity to inhibit TMPKmt and solely two 5′-modified thymidines were found to possess moderate inhibitory activity. In addition, a feasibility study of protecting groups for the 5-CH(2)OH moiety of 2′-deoxyuridines is described that enables to introduce the desired 5′-modification.

http://www.ncbi.nlm.nih.gov/pubmed/23199481