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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
1995-12-12
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pubmed:abstractText |
A series of amide derivatives of natural glycopeptide A-40,926 (A), its 6B-methyl ester (MA) and 6B-decarboxy-6B-hydroxymethyl derivative (RA) were prepared with the aim of obtaining activity against glycopeptide-resistant enterococci. These compounds are structurally related to a class of amides of 34-de(acetylglucosaminyl)-34-deoxy teicoplanin which showed interesting activity against strains of Enterococcus faecalis and E. faecium highly resistant to both vancomycin and teicoplanin. Among them, RA-amides MDL 63,246 and MDL 63,042 were the most active derivatives against several Gram-positive bacteria, including VanB and VanC enterococci, and were moderately active (MIC range 0.5 approximately 64 micrograms/ml) against strains of Enterococcus for which vancomycin and teicoplanin MICs were > or = 128 micrograms/ml. The chemical rationale and the synthesis of these new series of glycopeptide derivatives are described. Preliminary in vitro data are reported and structure-activity relationships are discussed.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0021-8820
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pubmed:author | |
pubmed:issnType |
Print
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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 |
869-83
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:7592033-Anti-Bacterial Agents,
pubmed-meshheading:7592033-Chromatography, High Pressure Liquid,
pubmed-meshheading:7592033-Drug Resistance, Microbial,
pubmed-meshheading:7592033-Enterococcus,
pubmed-meshheading:7592033-Magnetic Resonance Spectroscopy,
pubmed-meshheading:7592033-Microbial Sensitivity Tests,
pubmed-meshheading:7592033-Molecular Structure,
pubmed-meshheading:7592033-Structure-Activity Relationship,
pubmed-meshheading:7592033-Teicoplanin,
pubmed-meshheading:7592033-Vancomycin
|
pubmed:year |
1995
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pubmed:articleTitle |
New semisynthetic glycopeptides MDL 63,246 and MDL 63,042, and other amide derivatives of antibiotic A-40,926 active against highly glycopeptide-resistant VanA enterococci.
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pubmed:affiliation |
Marion Merrell Dow Research Institute, Lepetit Research Center, Gerenzano (Varese), Italy.
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pubmed:publicationType |
Journal Article,
Comparative Study
|