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Title: Synthesis and evaluation of 5-substituted 2 '-deoxyuridine monophosphate analogues as inhibitors of flavin-dependent thymidylate synthase in Mycobacterium tuberculosis
Authors: K√∂gler, Martin
Vanderhoydonck, Bart
De Jonghe, Steven
Rozenski, Jef
Van Belle, Kristien
Herman, Jean
Louat, Thierry
Parchina, Nastia
Sibley, Carol
Lescrinier, Eveline
Herdewijn, Piet # ×
Issue Date: Jul-2011
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:54 issue:13 pages:4847-4862
Abstract: A series of 5-substituted 2'-deoxyuridine monophosphate analogues has been synthesized and evaluated as potential inhibitors of mycobacterial ThyX, a novel flavin-dependent thymidylate synthase in Mycobacterium tuberculosis. A systematic SAR study led to the identification of compound 5a, displaying an IC50 value against mycobacterial ThyX of 0.91 mu M. This derivative lacks activity against the classical mycobacterial thymidylate synthase ThyA (IC50 > 50 mu M) and represents the first example of a selective mycobacterial FDTS inhibitor.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry
Interface Valorization Platform (IVAP) (-)
Laboratory of Experimental Transplantation
× corresponding author
# (joint) last author

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