rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
21
|
pubmed:dateCreated |
1999-12-9
|
pubmed:abstractText |
In the search for new ketolides with improved activities against erythromycin-resistant S. pneumoniae and H. influenzae we synthesized a new 11,12 carbamate ketolide substituted by an imidazo-pyridyl side chain: HMR 3647. This compound demonstrated a potent activity against erythromycin susceptible and resistant pathogens, including penicillin G/erythromycin A-resistant S. pneumoniae and H. influenzae. In vivo, HMR 3647 displayed good pharmacokinetic parameters (Cmax = 2.9 microg/ml, bioavailability=49%, AUC0.8 = 17.2 microg.h/l, t1/2=1h) and was shown to have a high therapeutic efficacy in mice infected by various respiratory pathogens, including multi-resistant S. pneumoniae and Gram negative bacteria such as H. influenzae. HMR 3647 appears to be a very promising agent for the treatment of respiratory infections and is currently in clinical trials.
|
pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Nov
|
pubmed:issn |
0960-894X
|
pubmed:author |
pubmed-author:AgouridasCC,
pubmed-author:AugerJ MJM,
pubmed-author:BenedettoCC,
pubmed-author:BonnefoyAA,
pubmed-author:BretinFF,
pubmed-author:ChantotJ FJF,
pubmed-author:D'AmbrièresS GSG,
pubmed-author:DenisAA,
pubmed-author:DussaratAA,
pubmed-author:FromentinCC,
pubmed-author:LachaudSS,
pubmed-author:LaurigWW,
pubmed-author:Le MartretOO,
pubmed-author:LoyauVV,
pubmed-author:PejacJ MJM,
pubmed-author:PerronSS,
pubmed-author:TessotNN
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pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
9
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
3075-80
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:10560728-Animals,
pubmed-meshheading:10560728-Anti-Bacterial Agents,
pubmed-meshheading:10560728-Drug Resistance, Microbial,
pubmed-meshheading:10560728-Erythromycin,
pubmed-meshheading:10560728-Gram-Negative Bacteria,
pubmed-meshheading:10560728-Gram-Positive Bacteria,
pubmed-meshheading:10560728-Haemophilus influenzae,
pubmed-meshheading:10560728-Ketolides,
pubmed-meshheading:10560728-Macrolides,
pubmed-meshheading:10560728-Mice,
pubmed-meshheading:10560728-Microbial Sensitivity Tests,
pubmed-meshheading:10560728-Molecular Structure
|
pubmed:year |
1999
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pubmed:articleTitle |
Synthesis and antibacterial activity of HMR 3647 a new ketolide highly potent against erythromycin-resistant and susceptible pathogens.
|
pubmed:affiliation |
Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France. alexis.denis@hmrag.com
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|