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Journal articles
Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase.
Abstract : We report on Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) inhibitory activities of a series of new 3'- and 5'-modified thymidine analogues including α- and β-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-α-thymidine analogue being the most active one (K(i)=0.17μM). This compound was capable of inhibiting mycobacteria growth at a concentration of 25μg/mL.
https://hal-pasteur.archives-ouvertes.fr/pasteur-00645423
Contributor : Hélène Munier-Lehmann Connect in order to contact the contributor
Submitted on : Monday, November 28, 2011 - 9:40:40 AM
Last modification on : Wednesday, November 3, 2021 - 2:56:48 PM
Contributor : Hélène Munier-Lehmann Connect in order to contact the contributor
Submitted on : Monday, November 28, 2011 - 9:40:40 AM
Last modification on : Wednesday, November 3, 2021 - 2:56:48 PM
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