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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2010-4-12
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1573-501X
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
215-24
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pubmed:meshHeading |
pubmed-meshheading:19484371-Adenosine Triphosphate,
pubmed-meshheading:19484371-Antimalarials,
pubmed-meshheading:19484371-Benzoic Acids,
pubmed-meshheading:19484371-Catechol O-Methyltransferase,
pubmed-meshheading:19484371-Humans,
pubmed-meshheading:19484371-Models, Molecular,
pubmed-meshheading:19484371-NAD,
pubmed-meshheading:19484371-Plasmodium falciparum,
pubmed-meshheading:19484371-Protozoan Proteins,
pubmed-meshheading:19484371-Trypanocidal Agents,
pubmed-meshheading:19484371-Trypanosoma brucei rhodesiense
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pubmed:year |
2010
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pubmed:articleTitle |
Parallel synthesis of a series of non-functional ATP/NAD analogs with activity against trypanosomatid parasites.
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pubmed:affiliation |
Institute of Pharmacy, Ernst-Moritz-Arndt-University, Friedrich-Ludwig-Jahn-Strasse 17, 17487, Greifswald, Germany. link@uni-greifswald.de
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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