rdf:type |
|
lifeskim:mentions |
umls-concept:C0005023,
umls-concept:C0008269,
umls-concept:C0024728,
umls-concept:C0032150,
umls-concept:C0036621,
umls-concept:C0080194,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243072,
umls-concept:C0332325,
umls-concept:C0962179,
umls-concept:C1883254,
umls-concept:C2717970
|
pubmed:issue |
1
|
pubmed:dateCreated |
2006-11-20
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pubmed:abstractText |
A targeted series of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives were synthesized and evaluated in vitro against the malarial cysteine protease falcipain-2 and a chloroquine resistant strain (W2) of Plasmodium falciparum. A novel series of 4-aminoquinoline semicarbazones were the most effective inhibitors of falcipain-2 (most potent inhibitor had IC(50)=0.63microM) while a bisquinoline semicarbazone compound 8f was the most potent antimalarial compound with an IC(50) of 0.07microM against W2. Compound 8f also weakly inhibited falcipain-2, with an IC(50) of 3.16microM, although its principal antiparasitic activity did not appear to be due to inhibition of this enzyme.
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pubmed:grant |
|
pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
0968-0896
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
15
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
273-82
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pubmed:dateRevised |
2007-12-3
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pubmed:meshHeading |
pubmed-meshheading:17052908-Animals,
pubmed-meshheading:17052908-Benzaldehydes,
pubmed-meshheading:17052908-Chloroquine,
pubmed-meshheading:17052908-Cysteine Endopeptidases,
pubmed-meshheading:17052908-Dose-Response Relationship, Drug,
pubmed-meshheading:17052908-Drug Resistance,
pubmed-meshheading:17052908-Mannich Bases,
pubmed-meshheading:17052908-Molecular Structure,
pubmed-meshheading:17052908-Parasitic Sensitivity Tests,
pubmed-meshheading:17052908-Phenols,
pubmed-meshheading:17052908-Plasmodium falciparum,
pubmed-meshheading:17052908-Stereoisomerism,
pubmed-meshheading:17052908-Structure-Activity Relationship,
pubmed-meshheading:17052908-Thiosemicarbazones
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum.
|
pubmed:affiliation |
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
|