Source:http://linkedlifedata.com/resource/pubmed/id/20116263
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2010-2-17
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pubmed:abstractText |
Betulin, a naturally occurring abundant triterpene is converted in four steps to 3,28-di-O-acetyllupa-12,18-diene. When various 4-substituted urazoles were oxidized to the corresponding urazines with iodobenzene diacetate in the presence of 3,28-di-O-acetyllupa-12,18-diene, new heterocyclic betulin derivatives were produced. These betulin derivatives were examined in a microplate assay at 50 microM for their ability to inhibit the growth of Leishmania donovani axenic amastigotes, a species that causes the fatal visceral leishmaniasis. GI(50) (concentration for 50% growth inhibition) values of the most effective compounds were determined and their cytotoxicity on the human macrophage cell line THP-1 evaluated. The anti-leishmanial activity on L. donovani amastigotes growing in macrophages was also examined. The heterocycloadduct between 3,28-di-O-acetyllupa-12,18-diene and 4-methylurazine was the most effective derivative with an GI(50)=8.9 microM against L. donovani amastigotes.
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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 |
Feb
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1573-82
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pubmed:meshHeading |
pubmed-meshheading:20116263-Animals,
pubmed-meshheading:20116263-Antiprotozoal Agents,
pubmed-meshheading:20116263-Cell Line,
pubmed-meshheading:20116263-Heterocyclic Compounds,
pubmed-meshheading:20116263-Humans,
pubmed-meshheading:20116263-Leishmania donovani,
pubmed-meshheading:20116263-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20116263-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:20116263-Triterpenes
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis and anti-leishmanial activity of heterocyclic betulin derivatives.
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pubmed:affiliation |
Division of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Helsinki, Finland.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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