1. Antibacterial and mechanism of action studies of boxazomycin A.
- Author
-
Singh SB, Occi J, Ondeyka J, Barrett JF, Masurekar P, Motyl M, Gill C, and Salituro G
- Subjects
- Animals, Mice, Protein Synthesis Inhibitors pharmacology, Drug Resistance, Bacterial drug effects, Anti-Bacterial Agents pharmacology, Anti-Bacterial Agents chemistry, Microbial Sensitivity Tests, Staphylococcal Infections drug therapy, Staphylococcal Infections microbiology, Staphylococcus aureus drug effects
- Abstract
Boxazomycins A-C are potent broad-spectrum antibiotics isolated from Actinomycetes strain G495-1 in 1987. We now report that boxazomycin A inhibits bacterial growth by selectively inhibiting protein synthesis, its effect is bacteriostatic, and it is equally active against drug resistant bacterial strains. No cross-resistance to protein synthesis inhibitors was observed suggesting that its inhibition is distinct from clinical protein synthesis inhibitors. We also report in vivo efficacy in a Staphylococcus aureus murine infection model supported by corresponding pharmacokinetic studies., (© 2024. Merck & Co., Inc., Rahway, NJ, USA and its affiliates, under exclusive licence to the Japan Antibiotics Research Association.)
- Published
- 2024
- Full Text
- View/download PDF