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Structural Basis for the Antibiotic Activity of Ketolides and Azalides [PDF]

Structure, 2003
The azalide azithromycin and the ketolide ABT-773, which were derived by chemical modifications of erythromycin, exhibit elevated activity against a number of penicillin- and macrolide-resistant pathogenic bacteria. Analysis of the crystal structures of the large ribosomal subunit from Deinococcus radiodurans complexed with azithromycin or ABT-773 ...
Frank Schlunzen, François Franceschi, Heike Bartels   +2 more
exaly   +4 more sources

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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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Effects of Macrolides and Ketolides on Mycobacterial Infections

Current Pharmaceutical Design, 2004
New macrolides, such as clarithromycin and azithromycin, are active agents to Mycobacterium avium complex (MAC). Both clarithromycin and azithromycin are well-known for the ability to improve the prognosis of AIDS patients with disseminated MAC infection.
Luiz E, Bermudez, Yoshitaka, Yamazaki
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[Macrolides and ketolides].

Enfermedades infecciosas y microbiologia clinica, 2010
Macrolides and ketolides are two families of antibiotics that share the same mechanism of action. They bind to different bases of the peptidyl transferase center of 23S RNA. The antibacterial spectrum of these drugs virtually overlaps, but dissimilarities in the affinity and number of binding sites results in differences in the intensity of their ...
Nazaret, Cobos-Trigueros, Oier, Ateka, Cristina, Pitart, Jordi, Vila   +3 more
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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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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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Review of Macrolides and Ketolides

Drugs, 2001
The first macrolide, erythromycin A, demonstrated broad-spectrum antimicrobial activity and was used primarily for respiratory and skin and soft tissue infections. Newer 14-, 15- and 16-membered ring macrolides such as clarithromycin and the azalide, azithromycin, have been developed to address the limitations of erythromycin.
G G, Zhanel, M, Dueck, D J, Hoban, L M, Vercaigne, J M, Embil, A S, Gin, J A, Karlowsky   +6 more
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ABT-773: a new ketolide antibiotic

Expert Opinion on Investigational Drugs, 2001
ABT-773 is a new semisynthetic derivative of erythromycin A, the ketolide class of broad spectrum antibacterial agents, in Phase II development by Abbott. With good broad spectrum activity against Gram-positive, some Gram-negative organisms and intracellular bacteria, ABT-773 is being developed as a respiratory agent. Structural changes in the ketolide
T J, Dougherty, J F, Barrett
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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, Xiaodong, Xu, Darren, Abbanat, Ellen Z, Baum, Barbara D, Foleno, Jamese J, Hilliard, Karen, Bush, Dennis J, Hlasta, Mark J, Macielag   +8 more
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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.
openaire   +3 more sources