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Molecules 2017, 22(3), 394;

In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria

School of Life Science, Handong Global University, Pohang 37554, Korea
LegoChem BioSciences. Inc., Daejeon 34302, Korea
School of Food Science and Biotechnology, Institute of Agricultural Science & Technology, Kyungpook National University, Daegu 41566, Korea
Author to whom correspondence should be addressed.
Academic Editor: Peter J. Rutledge
Received: 31 January 2017 / Revised: 21 February 2017 / Accepted: 2 March 2017 / Published: 3 March 2017
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Oxazolidinones are a novel class of synthetic antibacterial agents that inhibit bacterial protein synthesis. Here, we synthesized and tested a series of oxazolidinone compounds containing cyclic amidrazone. Among these compounds, we further investigated the antibacterial activities of LCB01-0648 against drug-susceptible or resistant Gram-positive cocci in comparison with those of six reference compounds. LCB01-0648 showed the most potent antimicrobial activities against clinically isolated Gram-positive bacteria. Against the methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant coagulase-negative staphylococci (MRCNS) isolates, LCB01-0648 showed the lowest MIC90s (0.5 mg/L) among the tested compounds. In addition, LCB01-0648 had the lowest minimum inhibitory concentrations (MICs) against the four linezolid-resistant S. aureus (LRSA) strains (range 2–4 mg/L). The results of the time–kill studies demonstrated that LCB01-0648 at a concentration 8× the (MIC) showed bactericidal activity against methicillin-susceptible Staphylococcus aureus MSSA or MRSA, but showed a bacteriostatic effect against LRSA. These results indicate that LCB01-0648 could be a good antibacterial candidate against multidrug-resistant (MDR) Gram-positive cocci. View Full-Text
Keywords: LCB01-0648; oxazolidinone; MICs; linezolid-resistant S. aureus LCB01-0648; oxazolidinone; MICs; linezolid-resistant S. aureus

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Oh, S.-H.; Kim, J.; Baek, S.-Y.; Chae, S.-E.; Park, H.-S.; Cho, Y.-L.; Kwak, J.-H. In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria. Molecules 2017, 22, 394.

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