Source:http://linkedlifedata.com/resource/pubmed/id/17095231
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2006-12-15
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pubmed:abstractText |
Bacterial FAS provides essential fatty acids for use in the assembly of key cellular components. Among them, FabI is an enoyl-ACP reductase which catalyzes the final and rate-limiting step of bacterial FAS. It is a potential target for selective antibacterial action, because it shows low overall sequence homology with mammalian enzymes. Until today, various compounds have been reported as inhibitors of bacterial FabI-inhibitory compounds. To discover novel small-molecular FabI inhibitors, we initially screened our compound library for inhibitory activity toward FabI of Escherichia coli. And discovered 4-pyridone derivatives as a lead compound. Structure optimization studies yielded 4-pyridone derivatives 7n having strong FabI-inhibitory and antibacterial activities against Staphylococcus aureus. There have been no reports concerning 4-pyridone derivatives as FabI inhibitor.
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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 |
Jan
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1106-16
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pubmed:meshHeading |
pubmed-meshheading:17095231-Enoyl-(Acyl-Carrier-Protein) Reductase (NADH),
pubmed-meshheading:17095231-Escherichia coli,
pubmed-meshheading:17095231-Indicators and Reagents,
pubmed-meshheading:17095231-Magnetic Resonance Spectroscopy,
pubmed-meshheading:17095231-Microbial Sensitivity Tests,
pubmed-meshheading:17095231-Pyridones,
pubmed-meshheading:17095231-Spectrometry, Mass, Fast Atom Bombardment,
pubmed-meshheading:17095231-Staphylococcus aureus,
pubmed-meshheading:17095231-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
4-Pyridone derivatives as new inhibitors of bacterial enoyl-ACP reductase FabI.
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pubmed:affiliation |
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd, 760 Morooka-cho, Kohoku-ku, Yokohama 222-8567, Japan.
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pubmed:publicationType |
Journal Article
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