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Structure-Activity Relationships for Six Ketolide Antibiotics

Current Microbiology, 2001
Six structurally related 3-keto-substituted macrolide antibiotics (ketolides) were compared for concentration-dependent inhibitory effects on growth rate, viable cell number, and protein synthesis rates in Staphylococcus aureus cells. Inhibitory effects on 50S ribosomal subunit formation were also examined, as this is a second target for these ...
Champney, W. Scott, Tober, Craig L.
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Telithromycin: An Oral Ketolide for Respiratory Infections

Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 2001
The ketolides represent a new subclass of antibiotics among the macrolide‐lincosamide‐streptogramin group. Telithromycin, the first ketolide to be awarded approvable status for clinical use, demonstrates in vitro activity against community‐acquired respiratory pathogens including penicillin‐ and erythromycin‐resistant Streptococcus pneumoniae.
D T, Bearden, M M, Neuhauser, K W, Garey
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[Telithromycin, first ketolide].

Revue medicale de Bruxelles, 2003
Telithromycine is the first ketolide on the market. Its characteristics are the two sites fixation on the bacterial ribosomia and and as a consequence a good activity on the majority of penicillin and macrolides resistant bacteria, included S. pneumonia and S. pyogenes.
Y, Van Laethem, J, Sternon
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Telithromycin (HMR 3647): The first ketolide antibiotic

Drugs of Today, 2001
Telithromycin, the first ketolide antibiotic to undergo clinical development, has been specifically designed to treat community-acquired respiratory tract infections, including those caused by resistant pathogens. Like macrolides, telithromycin inhibits protein synthesis by acting mainly on the 50S ribosomal subunit.
Yan-Qiong, Xiong, Thuan P., Le
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Macrolides and Ketolides

2013
Macrolides and ketolides are characterized by a very wide tissular distribution, which is related to their capacity to accumulate in the acidic compartments of the cells. This property is considered an advantage, because it concentrates the drug at the site of infection.
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Recent developments in macrolides and ketolides

Current Opinion in Microbiology, 1999
Emergence of bacterial resistance to macrolide antibiotics, particularly in Gram-positive bacteria, has been observed. Novel macrolides having C-4" carbamate functional groups and ketolides, the 3-keto derivatives of macrolides, have been found to have activities against macrolide-resistant strains.
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Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics

Bioorganic & Medicinal Chemistry Letters, 2004
AbstractFor Abstract see ChemInform Abstract in Full Text.
Todd C, Henninger   +8 more
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Macrolides and ketolides: azithromycin, clarithromycin, telithromycin

Infectious Disease Clinics of North America, 2004
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
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Ketolides in the treatment of respiratory infections

Expert Opinion on Pharmacotherapy, 2002
The ketolides are a new class of macrolides specifically designed to combat respiratory tract pathogens that have acquired resistance to macrolides. The ketolides are semi-synthetic derivatives of the 14-membered macrolide erythromycin A. There are currently two ketolides in the late stages of clinical development in the US (telithromycin [HMR-364 ...
George G, Zhanel, Daryl J, Hoban
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The Emerging New Generation of Antibiotic: Ketolides

Current Drug Targets - Infectious Disorders, 2001
The bacterial ribosome is a target for a variety of drug classes including macrolides. Macrolide antibiotics are primarily used for the treatment of respiratory tract infections. One of the most important features of the macrolide class is the excellent safety profile allowing the drug to be used broadly across all age groups.
P, Zhong, V, Shortridge
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