Source:http://linkedlifedata.com/resource/pubmed/id/17428097
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
2007-5-4
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pubmed:abstractText |
Fosmidomycin is the first representative of a new class of antimalarial drugs acting through inhibition of 1-deoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase (DXR), an essential enzyme in the non-mevalonate pathway for the synthesis of isoprenoids. This work describes a divergent strategy for the synthesis of a series of alpha-aryl-substituted fosmidomycin analogues, featuring a palladium-catalyzed Stille coupling as the key step. An alpha-(4-cyanophenyl)fosmidomycin analogue emerged as the most potent analogue in the present series. Its antimalarial activity clearly surpasses that of the reference compound fosmidomycin.
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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 |
May
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pubmed:issn |
0022-3263
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
72
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3783-9
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pubmed:meshHeading | |
pubmed:year |
2007
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pubmed:articleTitle |
Divergent strategy for the synthesis of alpha-aryl-substituted fosmidomycin analogues.
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pubmed:affiliation |
Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Belgium.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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