Glycopeptide antibiotics: from conventional molecules to new derivatives.

摘要: Vancomycin and teicoplanin are still the only glycopeptide antibiotics available for use in humans. Emergence of resistance enterococci staphylococci has led to restriction their severe infections caused by Gram-positive bacteria which no other alternative is acceptable (because or allergy). In parallel, considerable efforts have been made produce semisynthetic glycopeptides with improved pharmacokinetic pharmacodynamic properties, activity towards resistant strains. Several molecules now obtained, helping better delineate structure-activity relationships. Two being currently evaluated skin soft tissue phases II/III. The first, oritavancin (LY333328), 4'-chlorobiphenylmethyl derivative chloroeremomycin, an analogue vancomycin. It characterised by: i) a spectrum covering vancomycin-resistant (VRE), methicillin-resistant Staphylococcus aureus (MRSA) some extent glycopeptide-intermediate S. (GISA); ii) rapid bactericidal including against intracellular forms staphylococci; iii) prolonged half-life, allowing daily administration. second molecule dalbavancin (BI397), A40926. Dalbavancin similar that vancomycin-sensitive strains, but not active VRE. can be administered once week, based on its retention organism. Despite these remarkable potent agents should restricted infections, as older glycopeptides, extension poorly sensitive bacteria, limit risk potential selection resistance.