Patents on glycopeptides of the vancomycin family and their derivatives as antimicrobials: January 1999 – June 2003

The review summarises patents claiming novel glycopeptides of vancomycin and teicoplanin families published from January 1999 to June 2003. A brief overview of the structures of the most important natural antibacterial glycopeptides, the mode of action and resistance mechanism is presented. Structure–activity relationships for semisynthetic antibiotics are discussed and the structures and properties of novel clinically important compounds are presented. Semisynthetic derivatives containing various hydrophobic moieties were found to be active against glycopeptide-resistant bacteria. These compounds use a different or additional mechanism for antibacterial action to the parent antibiotics. These are not based on the interaction with Acyl-D-Ala-D-Ala or Acyl-D-Ala-D-lactate of the nascent bacterial peptidoglycan. Recently discovered antiviral activities of modified glycopeptides based on the interaction with viral receptors shows that glycopeptide derivatives are capable of interacting with membrane structures through mechanism(s) unrelated to -D-Ala-D-Ala or -D-Ala-D-lactate binding. Understanding the structural demands and the mechanics of this binding represents a challenge for researchers in this field.