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Antibiotic Resistance: Where Do Ketolides Fit?
Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 2002Burgeoning resistance to antibiotics among common respiratory pathogens poses a very real risk to public health. A need therefore exists for new antibiotics that not only target all common respiratory pathogens, including problematic strains such as penicillin‐ and macrolide‐resistant Streptococcus pneumoniae, but also resist resistance.
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Macrolides, Ketolides, and Glycylcyclines: Azithromycin, Clarithromycin, Telithromycin, Tigecycline
Infectious Disease Clinics of North America, 2009The 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 ...
Jerry M, Zuckerman +2 more
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Ketolides – The Modern Relatives of Macrolides
Clinical Pharmacokinetics, 2009As with other widely used antibacterials, the abundant use of macrolides for management of ambulant infections has promoted emergence of resistance against them. Ketolides are structurally related to macrolides and were developed to overcome macrolide resistance, while sharing pharmacodynamic and pharmacokinetic characteristics.
Zeitlinger, M, Wagner, C C, Heinisch, B
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Bioorganic & Medicinal Chemistry Letters, 2005
A series of new triazole-containing ketolides and 2-fluoro-ketolides in which the 5-O-desosamine was replaced by unnatural sugars were synthesized and evaluated against relevant macrolide-sensitive and macrolide-resistant respiratory pathogens. Excellent in vitro antibacterial activities were demonstrated for ketolide analogues having the 6'-OBz-3 ...
Chang-Hsing, Liang +9 more
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A series of new triazole-containing ketolides and 2-fluoro-ketolides in which the 5-O-desosamine was replaced by unnatural sugars were synthesized and evaluated against relevant macrolide-sensitive and macrolide-resistant respiratory pathogens. Excellent in vitro antibacterial activities were demonstrated for ketolide analogues having the 6'-OBz-3 ...
Chang-Hsing, Liang +9 more
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Macrolides, Azalides, and Ketolides
2011The macrolides and azalides are a generally well-tolerated class of antimicrobials used to treat several mild-to-moderate infections associated with Gram-positive microorganism. Over 50 years of clinical experience with the macrolides has also led to the observation of non-antimicrobial properties that are now being exploited in clinical practice.
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[Macrolides, ketolides and streptogramins].
Enfermedades infecciosas y microbiologia clinica, 2003Macrolides, ketolides and streptogramins are three families of antibiotics with different chemical structures, sharing the same mechanism of action. All three bind to distinct bases of the peptidyl transferase center of ARNr 23S. Their antibacterial spectrum practically overlaps, but dissimilarities in affinity and/or number of binding sites determine ...
José, Mensa +2 more
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Macrolide and Ketolide Resistance with Streptococcus pneumoniae
Medical Clinics of North America, 2006Antimicrobial agents in the macrolide family have long been considered drugs of potential utility in the management of infections caused by Streptococcus pneumoniae. However, with the emergence of macrolide resistance, the clinical value of macrolides in pneumococcal infections is threatened.
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Structure-activity relationships of ketolides vs. macrolides
Clinical Microbiology and Infection, 2008Since their discovery, the macrolide antimicrobials have proved clinically valuable for the treatment of respiratory tract infections, offering coverage against a broad spectrum of pathogens and excellent tolerability. However, the global increase in macrolide resistance among respiratory pathogens, particularly Streptococcus pneumoniae, threatens ...
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