Source:http://linkedlifedata.com/resource/pubmed/id/15785814
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
2005-3-23
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pubmed:abstractText |
5'-methylenearisteromycin 5 and its 2-fluoro derivative 6, which were designed as antimalarial agents because of their AdoHcy hydrolase inhibition, were synthesized from D-ribose, using a stereoselective intramolecular radical cyclization as the key step to construct the carbocyclic structure. These compounds were evaluated as AdoHcy hydrolase inhibitors with the recombinant human and malarial parasite enzymes. Although 5 and 6 were both potent inhibitors of the malarial parasite AdoHcy hydrolase, the 2-fluoro derivative 6 proved to be superior due to its lower inhibitory effect on the human enzyme. In addition, 6 was identified as a potent antimalarial agent using an in vitro assay system with Plasmodium falciparum.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1477-0520
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
3
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1245-51
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15785814-Adenosine,
pubmed-meshheading:15785814-Adenosylhomocysteinase,
pubmed-meshheading:15785814-Animals,
pubmed-meshheading:15785814-Antimalarials,
pubmed-meshheading:15785814-Inhibitory Concentration 50,
pubmed-meshheading:15785814-Magnetic Resonance Spectroscopy,
pubmed-meshheading:15785814-Mice,
pubmed-meshheading:15785814-Plasmodium falciparum,
pubmed-meshheading:15785814-Spectrometry, Mass, Fast Atom Bombardment
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pubmed:year |
2005
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pubmed:articleTitle |
Synthesis of 5'-methylenearisteromycin and its 2-fluoro derivative with potent antimalarial activity due to inhibition of the parasite S-adenosylhomocysteine hydrolase.
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pubmed:affiliation |
Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo, 060-0812, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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