Novel erythromycin derivatives with aryl groups tethered to the C-6 position are potent protein synthesis inhibitors and active against multidrug-resistant respiratory pathogens.

doi:10.1021/JM0102349

Paper

Novel erythromycin derivatives with aryl groups tethered to the C-6 position are potent protein synthesis inhibitors and active against multidrug-resistant respiratory pathogens.

Published Oct 18, 2001 · Zhenkun Ma, R. Clark, Antony A. Brazzale

Journal of medicinal chemistry

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108

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1

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Abstract

A novel series of erythromycin derivatives has been discovered with potent activity against key respiratory pathogens, including those resistant to erythromycin. These compounds are characterized by having an aryl group tethered to the C-6 position of the erythronolide skeleton. Extensive structural modification of the C-6 moiety led to the discovery of several promising compounds with potent activity against both mef- and erm-mediated resistant Streptoccoccus pneumoniae. Preliminary mechanistic studies indicated that the new macrolides are potent protein synthesis inhibitors, which interact with methylated ribosomes isolated from resistant organisms. In experimental animal models, these compounds exhibited excellent in vivo efficacy and balanced pharmacokinetic profiles.

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Novel erythromycin derivatives with aryl groups tethered to the C-6 position show potent activity against multidrug-resistant respiratory pathogens, with potential for use in antimicrobial therapy.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Novel erythromycin derivatives with aryl groups tethered to the C-6 position are potent protein synthesis inhibitors and active against multidrug-resistant respiratory pathogens.

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References

Citations

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Clarithromycin persists in soils after treatment, potentially promoting antibiotic resistance, with concentrations above 0.01 mg/kg increasing ermB gene abundance during the first week.

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1,2,3-triazole scaffolds can be effectively used in the development of novel, potent anti-MRSA agents to overcome drug resistance acquired by MRSA.

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