Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 24, Pages 7603-7611Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.10.021
Keywords
TMPKmt; Thymidine analogues; alpha- and beta-Nucleosides; Spectrophotometric binding assay; Inhibitory activity
Funding
- BOF, Ghent University
- Fund for Scientific Research-Flanders (F.W.O.-Vlaanderen)
- Institute for the Promotion of Innovation by Science and Technology in Flanders (IWT)
- Institut Pasteur (GPH Tuberculose, DAR-RI)
- CNRS
- INSERM
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We report on Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) inhibitory activities of a series of new 3'- and 5'-modified thymidine analogues including alpha- and beta-derivatives. In addition, several analogues were synthesized in which the 4-oxygen was replaced by a more lipophilic sulfur atom to probe the influence of this modification on TMPKmt inhibitory activity. Several compounds showed an inhibitory potency in the low micromolar range, with the 5'-arylthiourea 4-thio-alpha-thymidine analogue being the most active one (K(i) = 0.17 mu M). This compound was capable of inhibiting mycobacteria growth at a concentration of 25 mu g/mL. (C) 2011 Elsevier Ltd. All rights reserved.
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