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

Rational design of 5′-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Journal of medicinal chemistry - 02 Oct 2007

Van Daele I, Munier-Lehmann H, Froeyen M, Balzarini J, Van Calenbergh S

Link to Pubmed [PMID] – 17910427

J. Med. Chem. 2007 Nov;50(22):5281-92

Recently, thymidine monophosphate kinase (TMPK) emerged as an attractive target for developing inhibitors of Mycobacterium tuberculosis growth. The elucidation of the X-ray structure of TMPK of M. tuberculosis (TMPKmt), as well as the structure of an earlier serendipitously discovered dimeric thymidine inhibitor, laid the foundation for the design of potent and selective TMPKmt inhibitors reported here. Several hits identified within a series of 3′-C-branched thiourea-substituted beta-thymidine derivatives inspired us to construct a set of 5′-thiourea-substituted alpha-thymidine derivatives characterized by a similar relative orientation of the thymine and arylthiourea moieties. alpha-Thymidine derivative 15, featuring a (3-trifluoromethyl-4-chlorophenyl)thiourea moiety, has a Ki of 0.6 microM and a selectivity index of 600 versus human TMPK. Moreover, it represents the first TMPK inhibitor showing good inhibitory activity on growing M. bovis (MIC99 = 20 microg/mL) and M. tuberculosis (MIC50 = 6.25 microg/mL) strains.

http://www.ncbi.nlm.nih.gov/pubmed/17910427