In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria
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 aga...
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MDPI AG
2017-03-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/22/3/394 |
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| author | Sang-Hun Oh Josep Kim Sung-Yoon Baek Sang-Eun Chae Hee-Soo Park Young-Lag Cho Jin-Hwan Kwak |
| author_facet | Sang-Hun Oh Josep Kim Sung-Yoon Baek Sang-Eun Chae Hee-Soo Park Young-Lag Cho Jin-Hwan Kwak |
| author_sort | Sang-Hun Oh |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-20T06:19:36Z |
| format | Article |
| id | doaj.art-c0325a31ac484d03a38466944a346212 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-20T06:19:36Z |
| publishDate | 2017-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-c0325a31ac484d03a38466944a3462122022-12-21T19:50:27ZengMDPI AGMolecules1420-30492017-03-0122339410.3390/molecules22030394molecules22030394In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive BacteriaSang-Hun Oh0Josep Kim1Sung-Yoon Baek2Sang-Eun Chae3Hee-Soo Park4Young-Lag Cho5Jin-Hwan Kwak6School of Life Science, Handong Global University, Pohang 37554, KoreaSchool of Life Science, Handong Global University, Pohang 37554, KoreaLegoChem BioSciences. Inc., Daejeon 34302, KoreaLegoChem BioSciences. Inc., Daejeon 34302, KoreaSchool of Food Science and Biotechnology, Institute of Agricultural Science & Technology, Kyungpook National University, Daegu 41566, KoreaLegoChem BioSciences. Inc., Daejeon 34302, KoreaSchool of Life Science, Handong Global University, Pohang 37554, KoreaOxazolidinones 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.http://www.mdpi.com/1420-3049/22/3/394LCB01-0648oxazolidinoneMICslinezolid-resistant S. aureus |
| spellingShingle | Sang-Hun Oh Josep Kim Sung-Yoon Baek Sang-Eun Chae Hee-Soo Park Young-Lag Cho Jin-Hwan Kwak In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria Molecules LCB01-0648 oxazolidinone MICs linezolid-resistant S. aureus |
| title | In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria |
| title_full | In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria |
| title_fullStr | In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria |
| title_full_unstemmed | In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria |
| title_short | In Vitro Activities of LCB 01-0648, a Novel Oxazolidinone, against Gram-Positive Bacteria |
| title_sort | in vitro activities of lcb 01 0648 a novel oxazolidinone against gram positive bacteria |
| topic | LCB01-0648 oxazolidinone MICs linezolid-resistant S. aureus |
| url | http://www.mdpi.com/1420-3049/22/3/394 |
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