In-vitro and in-vivo evaluation of the antistaphylococcal activity of S-5556, a new 16-membered macrolide.

Abstract

During recent years, a resurgence of interest in the macrolides had led to the discovery of new derivatives of erythromycin with improved antibacterial activity and pharmacokinetic properties. In this study the in-vitro and in-vivo antistaphylococcal activity of S-5556, a 16-membered macrolide, was evaluated. In vitro, S-5556 was slightly less active than erythromycin against methicillin-susceptible Staphylococcus aureus. In contrast, it had superior activity for methicillin-resistant S. aureus (MRSA); several of these strains with inducible resistance to the macrolides-lincosamides-streptogramins group were susceptible to S-5556 whereas erythromycin was inactive. The combination of S-5556 with oxacillin was synergic for most MRSA strains tested. In vivo, a single prophylactic dose of S-5556 prevented 75%-100% of the cases of acute staphylococcal subcutaneous foreign body infection in a guinea pig-model. In a rat-model of chronic implant infection due to a methicillin- and erythromycin-resistant S. aureus strain, S-5556 significantly decreased the bacterial concentration around the foreign material, however resistant mutants emerged.

• Authors: C Chuard, P Rohner, V Dunand, R Auckenthaler, D P Lew
• Journal: The Journal of antimicrobial chemotherapy (J Antimicrob Chemother) Vol. 30 Issue 3 Pg. 327-37 (Sep 1992) ISSN: 0305-7453 [Print] England
• PMID: 1452498 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anti-Bacterial Agents
• Coagulase
• para-nitrobenzyl-oxime-tylosine
• Tylosin

Topics

• Animals
• Anti-Bacterial Agents (pharmacology)
• Coagulase (analysis)
• Disease Models, Animal
• Drug Synergism
• Foreign Bodies (complications)
• Guinea Pigs
• Methicillin Resistance
• Microbial Sensitivity Tests
• Rats
• Skin
• Species Specificity
• Staphylococcal Skin Infections (prevention & control)
• Staphylococcus aureus (drug effects, enzymology)
• Tylosin (analogs & derivatives, pharmacology)