Structure–activity relationships of ketolides vs. macrolides
نویسندگان
چکیده
منابع مشابه
Macrolides and ketolides: azithromycin, clarithromycin, telithromycin.
The advanced macrolides, azithromycin and clarithromycin, and the ketolide telithromycin are structural analogues of erythromycin. They have several distinct advantages when compared with erythromycin including enhanced spectrum of activity, more favorable pharmacokinetics and pharmacodynamics, once daily administration, and improved tolerability. This article reviews the pharmacokinetics, anti...
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The advanced macrolides, azithromycin and clarithromycin, and the ketolide, telithromycin, are structural analogs of erythromycin. They have several distinct advantages when compared with erythromycin, including enhanced spectrum of activity, more favorable pharmacokinetics and pharmacodynamics, once-daily administration, and improved tolerability. Clarithromycin and azithromycin are used exten...
متن کاملSAR of 11, 12-Carbamate Macrolides/Ketolides Linked With 1,4- Substituted-[1,2,3]-Triazoles
Structural features associated with ketolide antibiotics that may improve activity over their macrolide predecessors typically include: (1) lack of the 3-O-cladinose (2) presence of 3-keto group (3) the presence of heterocyte tethered to 11, 12-carbamate that interacts specifically with domain II of the bacterial rRNA. A novel compound library was designed to optimize domain II binding and anti...
متن کاملComparison of in vitro activities of ketolides, macrolides, and an azalide against the spirochete Borrelia burgdorferi.
Two ketolides, three macrolides, and one azalide were tested in vitro against 17 isolates of the B. burgdorferi s.l. complex. As measured in micrograms per milliliter, activity was highest for cethromycin (MIC at which 90% of the tested isolates were inhibited [MIC(90)], 0.0019 micro g/ml) and telithromycin (MIC(90), 0.0078 micro g/ml). Electron-microscope analysis and time-kill studies also su...
متن کاملPneumococcal resistance to macrolides, lincosamides, ketolides, and streptogramin B agents: molecular mechanisms and resistance phenotypes.
The macrolides, lincosamides, ketolides, and streptogramin B agents (the MLKS(B) antimicrobial agents) have related chemical structures and share similar molecular targets on the 50S ribosomal subunit of Streptococcus pneumoniae. Mutations in rRNA or ribosomal proteins generate a variety of resistance phenotypes. The M phenotype of S. pneumoniae, which predominates in North America, affords low...
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ژورنال
عنوان ژورنال: Clinical Microbiology and Infection
سال: 2001
ISSN: 1198-743X
DOI: 10.1046/j.1469-0691.2001.0070s3011.x