Structure-activity relationships for three macrolide antibiotics in Haemophilus influenzae

Current Microbiology
Susan MabeW Scott Champney

Abstract

A prior study examining differences in the activities of erythromycin and azithromycin on cellular functions in the Gram-negative pathogen, Haemophilus influenzae, revealed a marked difference in their inhibitory activities. The study revealed that protein synthesis and 50S ribosomal subunit assembly were equal targets for inhibition by azithromycin while erythromycin was a preferential inhibitor of translation. This contrast in inhibitory activities stimulated a comparative analysis of three additional antibiotics: clarithromycin, flurithromycin and roxithromycin. Each compound was tested over a concentration range for inhibitory effects on cellular processes. Clarithromycin was the most effective inhibitor of protein synthesis with an IC(50) of 5.6 microg/mL, followed by flurithromycin at 6 microg/mL, and roxithromycin at 9 microg/mL. IC(50) values for antibiotic effects on viable cell counts and growth rates were similar to those obtained for protein synthesis. Flurithromycin had the strongest effect on 50S ribosomal subunit formation with an IC(50) of 8 microg/mL, followed by clarithromycin and roxithromycin, at 9.0 microg/mL and 12.5 microg/mL respectively. 30S ribosomal subunit formation in cells treated with flurithromyc...Continue Reading

Citations

Nov 15, 2006·Antimicrobial Agents and Chemotherapy·Rafael SzczepanowskiAndreas Schlüter
Apr 25, 2006·Chemosphere·Franziska LangeClemens von Sonntag
Jan 17, 2008·Chemical Society Reviews·Sophie PurserVéronique Gouverneur
Jan 17, 2020·The Journal of Antimicrobial Chemotherapy·W Scott Champney
May 26, 2020·Journal of Biomolecular Structure & Dynamics·Yan ZhangWei Gu
Mar 10, 2021·Journal of Biomolecular Structure & Dynamics·Yu YangWei Gu
Oct 23, 2013·The Science of the Total Environment·Sudha Rani BatchuPiero R Gardinali

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