Source:http://linkedlifedata.com/resource/pubmed/id/21341744
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
2011-3-17
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pubmed:abstractText |
A novel class of potent direct 5-lipoxygenase (5-LO) inhibitors bearing a thiazolinone-scaffold identified by virtual screening is presented. A range of substitutions and the importance of the 2-phenyl moiety were evaluated. This series is characterized by high potency in intact polymorphonuclear leukocytes and a cell-free system, exemplified by (Z)-2-(4-chlorophenyl)-5-(4-methoxybenzylidene)-5H-thiazol-4-one (18, IC(50) = 0.28 and 0.09 ?M). These disubstituted thiazolinones may possess potential for intervention with inflammatory and allergic diseases and certain cancer types.
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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 |
Mar
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pubmed:issn |
1520-4804
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
24
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pubmed:volume |
54
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1943-7
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pubmed:meshHeading |
pubmed-meshheading:21341744-Arachidonate 5-Lipoxygenase,
pubmed-meshheading:21341744-Benzylidene Compounds,
pubmed-meshheading:21341744-Lipoxygenase Inhibitors,
pubmed-meshheading:21341744-Stereoisomerism,
pubmed-meshheading:21341744-Structure-Activity Relationship,
pubmed-meshheading:21341744-Thiazoles
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pubmed:year |
2011
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pubmed:articleTitle |
A class of 5-benzylidene-2-phenylthiazolinones with high potency as direct 5-lipoxygenase inhibitors.
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pubmed:affiliation |
Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, D-60438 Frankfurt, Germany. hofmann@pharmchem.uni-frankfurt.de
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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