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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2005-3-3
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pubmed:abstractText |
Fatty acid biosynthesis is essential for bacterial survival. Components of this biosynthetic pathway have been identified as attractive targets for the development of new antibacterial agents. FabH, beta-ketoacyl-ACP synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-positive and -negative bacteria. Small molecules that inhibit FabH enzymatic activity have the potential to be candidates within a novel class of selective, nontoxic, broad-spectrum antibacterials. Using crystallographic structural information on these highly conserved active sites and structure based drug design principles, a benzoylaminobenzoic acid series of compounds was developed as potent inhibitors of FabH. This inhibitor class demonstrates strong antibacterial activity against Gram-positive and selected Gram-negative organisms.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AppeltKrzysztofK,
pubmed-author:ChuShaosongS,
pubmed-author:CortezJosephJ,
pubmed-author:GajiwalaKetan SKS,
pubmed-author:LuJiaJ,
pubmed-author:MargosiakStephenS,
pubmed-author:NieZheZ,
pubmed-author:NikulinVictorV,
pubmed-author:PerrettaCarinC,
pubmed-author:SuYingY,
pubmed-author:YagerKraig MKM
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1596-609
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pubmed:dateRevised |
2010-10-7
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pubmed:meshHeading |
pubmed-meshheading:15743201-3-Oxoacyl-(Acyl-Carrier-Protein) Synthase,
pubmed-meshheading:15743201-Anti-Bacterial Agents,
pubmed-meshheading:15743201-Bacterial Proteins,
pubmed-meshheading:15743201-Combinatorial Chemistry Techniques,
pubmed-meshheading:15743201-Crystallization,
pubmed-meshheading:15743201-Drug Design,
pubmed-meshheading:15743201-Gram-Negative Bacteria,
pubmed-meshheading:15743201-Gram-Positive Bacteria,
pubmed-meshheading:15743201-Microbial Sensitivity Tests,
pubmed-meshheading:15743201-Models, Molecular,
pubmed-meshheading:15743201-Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.
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pubmed:affiliation |
Departments of Medicinal Chemistry, Protein Biochemistry and Structural Biology, Quorex Pharmaceuticals Inc., 1890 Rutherford Road, Suite 200, Carlsbad, CA 92008, USA. zhenie@phoenixpharmaco.com
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pubmed:publicationType |
Journal Article
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