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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2008-4-4
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pubmed:abstractText |
Although earlier pleuromutilin analogues showed potent in vitro antibacterial activity against some Gram-positive pathogens, their in vivo efficacy was low because of insufficient pharmacokinetic properties. We designed novel thioether pleuromutilin derivatives having a purine ring as a polar and water solubilizing group and identified a promising pleuromutilin analogue 6 with good solubility in water ( approximately 50 mg/mL). Compound 6 exhibited excellent in vitro and in vivo antibacterial activity against some Gram-positive strains, including drug-resistant pathogens.
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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 |
Apr
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1991-4
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pubmed:meshHeading |
pubmed-meshheading:18330977-Animals,
pubmed-meshheading:18330977-Anti-Bacterial Agents,
pubmed-meshheading:18330977-Disease Models, Animal,
pubmed-meshheading:18330977-Diterpenes,
pubmed-meshheading:18330977-Dose-Response Relationship, Drug,
pubmed-meshheading:18330977-Drug Design,
pubmed-meshheading:18330977-Drug Resistance, Bacterial,
pubmed-meshheading:18330977-Gram-Negative Bacteria,
pubmed-meshheading:18330977-Gram-Positive Bacteria,
pubmed-meshheading:18330977-Gram-Positive Bacterial Infections,
pubmed-meshheading:18330977-Mice,
pubmed-meshheading:18330977-Microbial Sensitivity Tests,
pubmed-meshheading:18330977-Molecular Structure,
pubmed-meshheading:18330977-Solubility,
pubmed-meshheading:18330977-Stereoisomerism,
pubmed-meshheading:18330977-Water
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pubmed:year |
2008
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pubmed:articleTitle |
Water-soluble pleuromutilin derivative with excellent in vitro and in vivo antibacterial activity against gram-positive pathogens.
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pubmed:affiliation |
Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co. Ltd., Enoki 33-94, Suita, Osaka, 564-0053, Japan.
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pubmed:publicationType |
Journal Article
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