Modified 5'-trityl nucleosides as inhibitors of Plasmodium falciparum dUTPase

Ruda, G. F. and Nguyen, C. and Ziemkowski, P. and Felczak, K. and Kasinathan, G. and Musso-Buendia A., and Sund, C. and Zhou, X. X. and Kaiser, M. and Ruiz-Perez L. M., and Brun, R. and Kulikowski, T. and Johansson, N. G. and Gonzalez-Pacanowska D., and Gilbert, I. H.. (2011) Modified 5'-trityl nucleosides as inhibitors of Plasmodium falciparum dUTPase. ChemMedChem : chemistry enabling drug discovery, Vol. 6, H. 2. pp. 309-320.

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Official URL: http://edoc.unibas.ch/dok/A6002275

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2'-Deoxyuridine triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for the treatment of malaria. We previously reported the discovery of 5'-tritylated analogues of deoxyuridine as selective inhibitors of this Plasmodium falciparum enzyme. Herein we report further structure-activity studies; in particular, variations of the 5'-trityl group, the introduction of various substituents at the 3'-position of deoxyuridine, and modifications of the base. Compounds were tested against both the enzyme and the parasite. Variations of the 5'-trityl group and of the 3'-substituent were well tolerated and yielded active compounds. However, there is a clear requirement for the uracil base for activity, because modifications of the uracil ring result in loss of enzyme inhibition and significant decreases in antiplasmodial action
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:08 Nov 2012 16:22
Deposited On:08 Nov 2012 16:09

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