Molecules 2017, 22(12), 2096; https://doi.org/10.3390/molecules22122096
In Vivo Activity of LCB 01-0699, a Prodrug of LCB 01-0648, against Staphylococcus aureus
1
School of Life Science, Handong Global University, Pohang 37554, Korea
2
Institute of Agricultural Science & Technology, School of Food Science and Biotechnology, Kyungpook National University, Daegu 41566, Korea
3
LegoChem BioSci. Inc., Daejeon 34302, Korea
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These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 10 November 2017 / Revised: 23 November 2017 / Accepted: 28 November 2017 / Published: 29 November 2017
(This article belongs to the Collection Antibiotics & Superbugs: New Strategies to Combat Antimicrobial Resistance)
Abstract
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. View Full-TextKeywords:
LCB01-0699; LCB01-0648; oxazolidinone; in vivo activity; skin infection
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Oh, S.-H.; Park, H.-S.; Lee, J.-H.; Baek, S.-Y.; Chae, S.-E.; Oh, K.; Cho, Y.L.; Kwak, J.-H. In Vivo Activity of LCB 01-0699, a Prodrug of LCB 01-0648, against Staphylococcus aureus. Molecules 2017, 22, 2096.
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