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Molecules 2017, 22(3), 394; doi:10.3390/molecules22030394

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

1
School of Life Science, Handong Global University, Pohang 37554, Korea
2
LegoChem BioSciences. Inc., Daejeon 34302, Korea
3
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
View Full-Text   |   Download PDF [1152 KB, uploaded 3 March 2017]   |  

Abstract

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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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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