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Parallel synthesis of a series of non-functional ATP/NAD analogs with activity against trypanosomatid parasites

Link, Andreas and Heidler, Philipp and Kaiser, Marcel and Brun, Reto. (2010) Parallel synthesis of a series of non-functional ATP/NAD analogs with activity against trypanosomatid parasites. Molecular Diversity, 14 (2). pp. 215-224.

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Official URL: http://edoc.unibas.ch/dok/A5842972

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Abstract

Non-functional analogs of the cofactors ATP and NAD are putative inhibitors of ATP- or NAD-dependant enzymes. Since pathogenic protozoa rely heavily on the salvage of purine nucleosides from the bloodstream of their host, such compounds are of interest as antiplasmodial and antitrypanosomal agents with a multitude of molecular targets. By replacing the negatively charged phosphate residues with a constrained unsaturated amide spacer and the nicotinamide moiety of NAD with various lipophilic substituents, 15 new ATP/NAD analogs were obtained in screening quantities. In these compounds, a 5'-desoxyadenosine moiety was conserved as key molecular recognition motif. The inhibition of P. falciparum and T. brucei ssp. in a whole parasite in vitro assay is reported
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
Bibsysno:Link to catalogue
Publisher:Springer
ISSN:1381-1991
e-ISSN:1573-501X
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:28 Nov 2017 10:31
Deposited On:14 Sep 2012 06:46

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