In Vivo Activity of LCB 01-0699, a Prodrug of LCB 01-0648, against Staphylococcus aureus

• Main Authors: Sang-Hun Oh, Hee-Soo Park, Jun-Hyung Lee, Sung-Yun Baek, Sang-Eun Chae, Kyuman Oh, Young Lag Cho, Jin-Hwan Kwak
• Format: Article
• Language: English
• Published: MDPI AG 2017-11-01
• Series: Molecules
• Subjects: LCB01-0699; LCB01-0648; oxazolidinone; in vivo activity; skin infection
• Online Access: https://www.mdpi.com/1420-3049/22/12/2096

LCB01-0648 is a novel oxazolidinone compound that shows potent antibacterial activities against most Gram-positive cocci, including the multi-drug resistant Staphylococcus aureus. 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.