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Molecules ; 22(12)2017 Nov 29.
Article in English | MEDLINE | ID: mdl-29186032

ABSTRACT

LCB01-0648 is a novel oxazolidinone compound that shows potent antibacterial activities against most Gram-positive cocci, including the multi-drug resistant Staphylococcusaureus. In this study, in vivo activity of LCB01-0699, a LCB01-0648 prodrug, against S.aureus was evaluated in comparison with that of Linezolid. The results of the systemic infection study demonstrated that LCB01-0699 was more potent than Linezolid against methicillin-susceptible and -resistant S. aureus strains. The in vivo efficacy of LCB01-0699 against methicillin-susceptible and -resistant S. aureus strains in a skin infection model showed more potent activity than Linezolid. LCB01-0699 shows potent in vivo activity against methicillin-susceptible and -resistant S. aureus strains, suggesting that LCB01-0699 would be a novel candidate for the treatment of these infectious diseases caused by S. aureus.


Subject(s)
Anti-Bacterial Agents/pharmacology , Prodrugs/pharmacology , Staphylococcus aureus/drug effects , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacokinetics , Anti-Bacterial Agents/therapeutic use , Female , Mice , Microbial Sensitivity Tests , Oxazolidinones/chemistry , Oxazolidinones/pharmacology , Oxazolidinones/therapeutic use , Prodrugs/chemistry , Prodrugs/pharmacokinetics , Prodrugs/therapeutic use , Staphylococcal Infections/drug therapy , Staphylococcal Infections/microbiology
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