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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2011-1-17
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pubmed:abstractText |
Compounds inhibiting LpxC in the lipid A biosynthetic pathway are promising leads for novel antibiotics against multidrug-resistant Gram-negative pathogens. We report the syntheses and structural and biochemical characterizations of LpxC inhibitors based on a diphenyl-diacetylene (1,4-diphenyl-1,3-butadiyne) threonyl-hydroxamate scaffold. These studies provide a molecular interpretation for the differential antibiotic activities of compounds with a substituted distal phenyl ring as well as the absolute stereochemical requirement at the C2, but not C3, position of the threonyl group.
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pubmed:grant |
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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 |
Jan
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pubmed:issn |
1464-3391
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pubmed:author |
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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 |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
852-60
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pubmed:dateRevised |
2011-5-24
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pubmed:meshHeading |
pubmed-meshheading:21194954-Amidohydrolases,
pubmed-meshheading:21194954-Amino Acid Sequence,
pubmed-meshheading:21194954-Anti-Bacterial Agents,
pubmed-meshheading:21194954-Binding Sites,
pubmed-meshheading:21194954-Computer Simulation,
pubmed-meshheading:21194954-Enzyme Inhibitors,
pubmed-meshheading:21194954-Escherichia coli,
pubmed-meshheading:21194954-Escherichia coli Proteins,
pubmed-meshheading:21194954-Microbial Sensitivity Tests,
pubmed-meshheading:21194954-Molecular Sequence Data,
pubmed-meshheading:21194954-Protein Structure, Tertiary,
pubmed-meshheading:21194954-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold.
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pubmed:affiliation |
Department of Chemistry, Jilin University, Changchun, PR China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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