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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2001-11-15
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pubmed:abstractText |
A novel series of erythromycin derivatives has been discovered with potent activity against key respiratory pathogens, including those resistant to erythromycin. These compounds are characterized by having an aryl group tethered to the C-6 position of the erythronolide skeleton. Extensive structural modification of the C-6 moiety led to the discovery of several promising compounds with potent activity against both mef- and erm-mediated resistant Streptoccoccus pneumoniae. Preliminary mechanistic studies indicated that the new macrolides are potent protein synthesis inhibitors, which interact with methylated ribosomes isolated from resistant organisms. In experimental animal models, these compounds exhibited excellent in vivo efficacy and balanced pharmacokinetic profiles.
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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 |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AlderJJ,
pubmed-author:BrazzaleAA,
pubmed-author:CaoZZ,
pubmed-author:ChuD TDT,
pubmed-author:ClarkR FRF,
pubmed-author:EwingPP,
pubmed-author:FlammRR,
pubmed-author:GriesgraberGG,
pubmed-author:LORR,
pubmed-author:LuGG,
pubmed-author:MeulbroekJJ,
pubmed-author:MitterAA,
pubmed-author:NemotoP APA,
pubmed-author:NiliusA MAM,
pubmed-author:OrY SYS,
pubmed-author:PhanL TLT,
pubmed-author:PlattnerJ JJJ,
pubmed-author:RuppM JMJ,
pubmed-author:ShortridgeV DVD,
pubmed-author:WangSS,
pubmed-author:YongHH,
pubmed-author:ZhangSS,
pubmed-author:ZhangXX,
pubmed-author:ZhongPP
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4137-56
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:11708916-Animals,
pubmed-meshheading:11708916-Anti-Bacterial Agents,
pubmed-meshheading:11708916-Carbamates,
pubmed-meshheading:11708916-Cell-Free System,
pubmed-meshheading:11708916-Drug Resistance, Multiple,
pubmed-meshheading:11708916-Erythromycin,
pubmed-meshheading:11708916-Haemophilus influenzae,
pubmed-meshheading:11708916-Ketolides,
pubmed-meshheading:11708916-Lung,
pubmed-meshheading:11708916-Mice,
pubmed-meshheading:11708916-Models, Molecular,
pubmed-meshheading:11708916-Protein Biosynthesis,
pubmed-meshheading:11708916-Protein Synthesis Inhibitors,
pubmed-meshheading:11708916-Rats,
pubmed-meshheading:11708916-Respiratory Tract Infections,
pubmed-meshheading:11708916-Ribosomes,
pubmed-meshheading:11708916-Staphylococcus aureus,
pubmed-meshheading:11708916-Streptococcus pneumoniae,
pubmed-meshheading:11708916-Streptococcus pyogenes,
pubmed-meshheading:11708916-Structure-Activity Relationship,
pubmed-meshheading:11708916-Transcription, Genetic
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pubmed:year |
2001
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pubmed:articleTitle |
Novel erythromycin derivatives with aryl groups tethered to the C-6 position are potent protein synthesis inhibitors and active against multidrug-resistant respiratory pathogens.
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pubmed:affiliation |
Infectious Disease Research, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, Illinois 60064-3537, USA. zhenkun.ma@abbott.com
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pubmed:publicationType |
Journal Article
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