Source:http://linkedlifedata.com/resource/pubmed/id/17608397
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
15
|
pubmed:dateCreated |
2007-7-19
|
pubmed:abstractText |
Five adamantyl-containing carboxamides of eremomycin or vancomycin were synthesized and their antibacterial activities against some Gram-positive clinical isolates were investigated in vitro and in vivo. The adamantyl-2 amide of glycopeptide antibiotic eremomycin (1a in Chart 1, AN0900) was the most active compound and showed high activity against several Gram-positive pathogens: vancomycin-susceptible staphylococci and enterococci, glycopeptide-intermediate-resistant Staphylococcus aureus, and glycopeptide-resistant enterococci. Compound 1a was equally active in vitro against both Ciprofloxacin-susceptible and -resistant Bacillus anthracis strains (MICs 0.25-0.5 microg/mL). It was distinguished by having a 2.8 h half-life (t1/2) in mice and a volume of distribution of 2.18 L/kg. Compound 1a was active against Staphylococcus aureus in mice (iv) and provided complete protection against a lethal intravenous challenge with vegetative B. anthracis bacilli and also in a murine pulmonary anthrax model in which mice were challenged with Bacillus anthracis spores.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jul
|
pubmed:issn |
0022-2623
|
pubmed:author |
pubmed-author:ChuDanielD,
pubmed-author:HeineHenryH,
pubmed-author:IpEmilyE,
pubmed-author:LovchikJulieJ,
pubmed-author:LyonsC RichardCR,
pubmed-author:MaplesKirk RKR,
pubmed-author:OlsufyevaEvgenia NEN,
pubmed-author:PlattnerJacob JJJ,
pubmed-author:PreobrazhenskayaMaria NMN,
pubmed-author:PrintsevskayaSvetlana SSS,
pubmed-author:SolovievaSvetlana ESE,
pubmed-author:WheelerConradC,
pubmed-author:ZhangYong-KangYK
|
pubmed:issnType |
Print
|
pubmed:day |
26
|
pubmed:volume |
50
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
3681-5
|
pubmed:meshHeading |
pubmed-meshheading:17608397-Animals,
pubmed-meshheading:17608397-Anthrax,
pubmed-meshheading:17608397-Anti-Bacterial Agents,
pubmed-meshheading:17608397-Bacillus anthracis,
pubmed-meshheading:17608397-Drug Resistance, Bacterial,
pubmed-meshheading:17608397-Glycopeptides,
pubmed-meshheading:17608397-Gram-Positive Bacteria,
pubmed-meshheading:17608397-Mice,
pubmed-meshheading:17608397-Microbial Sensitivity Tests,
pubmed-meshheading:17608397-Staphylococcal Infections,
pubmed-meshheading:17608397-Staphylococcus aureus,
pubmed-meshheading:17608397-Structure-Activity Relationship
|
pubmed:year |
2007
|
pubmed:articleTitle |
Novel semisynthetic derivative of antibiotic Eremomycin active against drug-resistant gram-positive pathogens including Bacillus anthracis.
|
pubmed:affiliation |
Anacor Pharmaceuticals, Inc., 1060 East Meadow Circle, Palo Alto, California 94303, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.
|