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Antimicrobial Activities of LCB01-0183, a New Oxazolidinone  

Lee, Hyun-Hee (School of Life Science, Handong Global University)
Jung, Sung-Ji (School of Life Science, Handong Global University)
Jeong, Ji-Woong (School of Life Science, Handong Global University)
Cho, Young-Lag (LegoChem BioScience, Inc.)
Kim, Yong-Zu (LegoChem BioScience, Inc.)
Kwak, Jin-Hwan (School of Life Science, Handong Global University)
Publication Information
YAKHAK HOEJI / v.57, no.2, 2013 , pp. 95-100 More about this Journal
Abstract
This study was performed to analyze in vitro and in vivo activities of LCB01-0183, a new oxazolidinone, against clinical isolates of bacteria. In vitro antibacterial activity of LCB01-0183 was tested by the two fold agar dilution method. In vivo activity of LCB01-0183 was determined against systemic infections in mice. LCB01-0183 showed most potent activity among the test compounds against clinical isolates of Gram-positive bacteria. Furthermore, the protective activity of LCB01-0183 was very effective against systemic infections in mice by oral or subcutaneous administration. In time kill study, LCB01-0183 showed a bacteriostatic activity during 24 hours. LCB01-0183 had potent in vitro and in vivo activity against Gram-positive bacteria including drug-resistant strains.
Keywords
LCB01-0183; antibacterial activity; MIC; time-kill; oxazolidinone;
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1 Lobritz, M., Hutton-Thomas, R., Marshall, S. and Rice, L. B. : Recombination proficiency influences frequency and locus of mutational resistance to linezolid in Enterococcus faecalis. Antimicrob. Agents. Chemother. 47, 3318 (2003).   DOI
2 Mendes, R. E., Deshpande, L. M., Castanheira, M., DiPersio, J., Saubolle, M. A. and Jones, R. N. : First report of cfrmediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States. Antimicrob. Agents. Chemother. 52, 2244 (2008).   DOI   ScienceOn
3 Diekema, D. J. and Jones, R. N. : Oxazolidinone antibiotics. Lancet 358, 1975 (2001).   DOI   ScienceOn
4 Michael, A. F. and Christopher, T. W. : Antibiotics for emerging pathogens. Science 325, 1089 (2009).   DOI   ScienceOn
5 Sreenivas, K., Amarnath, P. V. S., Mallik, A., Sarnaik, H., Selva Kumar, N., Takhi, M., Trehan, S., Sitaram Kumar, M., Iqbal, J., Rajagopalan, R. and Chakrabarti, R. : In vitro and in vivo antibacterial evaluation of DRF 8417, a new oxazolidinone. J. Antimicrob. Chemother. 60, 159 (2007).   DOI   ScienceOn
6 Levy, S. B. and Marshall, B. : Antibacterial resistance worldwide: causes, challenges and responses. Nature. Med. 10, s122 (2004).   DOI   ScienceOn
7 Noskin, G. A., Siddiqui, F., Stosor, V., Hacek, D. and Peterson, L. R. : In vitro activities of linezolid against important Grampositive bacterial pathogens including vancomycin-resistant Enterococci. Antibicrob. Agents. Chemother. 43, 2059 (1999).
8 Vara Prasad, J. V. : New oxazolidinones. Curr. Opin. Microbiol. 10, 454 (2007).   DOI   ScienceOn
9 Swaney, S. M., Aoki, H., Ganoza, M. C. and Shinabarger, D. L. : The oxazolidinone linezollid inhibits initiation of protein synthesis in bacteria. Antimicrob. Agents. Chemother. 42, 3251 (1998).
10 Gill, C. J., Abruzzo, G. K., Flattery, A. M., Misura, A. S., Bartizal, K. and Hickey, E. J. : In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection. Antimicrob. Agents. Chemother. 51, 3434 (2007).   DOI   ScienceOn
11 Lin, A. H., Murray, R. W., Vidamar, T. J. and Marotti, K. R. : The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob. Agents. Chemother. 41, 2127 (1997).
12 Jones, R. N., Ross, J. E., Castanheira, M. and Mendes, R. E. : United States resistance surveillance results for linezolid (LEADER Program for 2007). Diagn. Microbiol. Infect. Dis. 62, 416 (2008).   DOI   ScienceOn
13 Shaw, K. J., Poppe, S., Schaadt, R., Brown-Driver, V., Finn, J., Pillar, C. M., Shinabarger, D. and Zurenko, G. : In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains. Antimicrob. Agents. Chemother. 52, 4442 (2008).   DOI   ScienceOn
14 Leach, K. L., Swaney, S. M., Colca, J. R., McDonald, W. G., Blinn, J. R., Thomasco, L. M., Gadwood, R. C., Shinabarger, D., Xiong, L. and Mankin, A. S. : The site of action of oxazolidinone antibiotics in living bacteria and in human mitochondria. Mol. Cell. 26, 393 (2007).   DOI   ScienceOn
15 Moise, P. A., Forrest, A., Birmingham, M. C. and Schentag, J. J. : The efficacy and safety of linezolid as treatment for Staphylococcus aureus infections in compassionate use patients who are intolerant of, or who have failed to respond to vancomycin. J. Antimicrob. Chemother. 50, 1017 (2002).   DOI   ScienceOn
16 Meka, V. G. and Gold, H. S. : Antimicrobial resistance to linezolid. Clin. Infect. Dis. 39, 1010 (2004).   DOI   ScienceOn
17 Clinical and Laboratory Standards Institute (CLSI) : Performance Standards for Antimicrobial Susceptibility Testing; 21th Informational Supplement. CLSI Document M100-S22. CLSI, Wayne, PA (2012).
18 Clinical and Laboratory Standards Institute (CLSI) : Methods for Determining Bactericidal Activity of Antimicrobial Agents. CLSI document M26-A. CLSI, Wayne, PA (1999).
19 Bliss, C. I. : Statistics in bioassay. Academic Press, Inc., New York (1985).
20 Spellberg, B., Powers, J. H., Brass, E. P., Miller, L. G. and Edwards, J. E. Jr. : Trends in antimicrobial drug development implications for the future. Clin. Infect. Dis. 38, 1279 (2004).   DOI   ScienceOn
21 Luh, K. T., Hsueh, P. R., Teng, L. J., Pan, H. J., Chen, Y. C., Lu, J. J., Wu, J. J. and Ho, S. W. : Quinupristin-dalfopristin resistance among Gram-positive bacteria in Taiwan. Antimicrob. Agents. Chemother. 44, 3374 (2004).