Antibacterial activity of LCB01-0062, a novel oxazolidinone

Jung, Sung-Ji; Yun, I. Na Rae; Park, Hee Soo; Lee, Hyun‐Hee; Jeong, Ji-Woong; Kim, Yong-Zu; Cho, Young Lag; Kwak, Jin‐Hwan

doi:10.1016/j.ijantimicag.2012.07.017

Cited by 7 publications

(5 citation statements)

References 10 publications

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“…Previously, we synthesized novel oxazolidinones including LCB01-0062 and LCB01-0371 [ 40 , 41 ]. These oxazolidinones showed potent in vitro and in vivo activities against most Gram-positive cocci.…”

Section: Discussionmentioning

confidence: 99%

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

Kim

Baek³

et al. 2017

Molecules

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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.

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Section: Discussionmentioning

confidence: 99%

“…Previously, we reported novel oxazolidinone compounds such as LCB01-0062 and LCB01-0371 which showed potent antibacterial activities against most Gram-positive cocci [ 40 , 41 ]. While LCB01-0371 has high potency and safety, this oxazolidinone showed moderate activity against linezolid-resistant strains [ 41 ].…”

Section: Introductionmentioning

confidence: 99%

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

Kim

Baek³

et al. 2017

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“…LegoChem Biosciences, Inc. (Daejeon, South Korea) has developed several oxazolidinone derivatives as antibacterial agents in the last decade. 32–35 For example, compound 13 (LCB01-0062) (Fig. 2) showed in vitro activity against clinical isolates of Gram-positive bacteria compared to several antibacterial drugs, including linezolid, erythromycin, ciprofloxacin, and vancomycin.…”

Section: Oxazolidinones As Antibacterial Agentsmentioning

confidence: 99%

“…Furthermore, in vivo studies in a mouse model of infection caused by S. aureus Giorgio (methicillin-susceptible) showed that compound 13 was more active than linezolid. 35 Compound 14 (LCB 01-0648) ( Fig. 2 ) is another representative that was developed after a lead optimization campaign on delpazolid (7) (LCB01-0371).…”

Section: Oxazolidinones As Antibacterial Agentsmentioning

confidence: 99%

Oxazolidinones as versatile scaffolds in medicinal chemistry

et al. 2023

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“…The currently developed oxazolidinones such as tedizolid (TR-701), LCB01-0062, DA-7218, and DA-7157 have been reported to be more potent and/or exhibit lower toxicity than linezolid (11)(12)(13). On comparing the difference in the structure and activity between sy142 and linezolid, it could be concluded that the N-heteroaryl group at the 4-position of piperazine is favorable for enhancing the activity of sy142.…”

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In Vitro Activity of Novel Oxazolidinone Analogs and 13 Conventional Antimicrobial Agents against Clinical Isolates of Staphylococcus aureus in Beijing, China

et al. 2014

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SUMMARY: Methicillin-resistant Staphylococcus aureus (MRSA) has been a public health concern since it was first identified in the United Kingdom in 1961. In this study, we investigated the prevalence of MRSA in the PLA 309 Hospital located in Beijing, China, and we determined the susceptibility of S. aureus to novel oxazolidinone analogs and 13 conventional antimicrobial agents. It was shown that drug resistant patterns were severe among the clinical isolates, and the average rate of MRSA among the S. aureus strains was 56.3z. All the S. aureus strains tested were completely susceptible to linezolid, but the minimum inhibitory concentration distribution drifted upwards. Among the novel oxazolidinone analogs, sy142 exhibited more potent antimicrobial activity than linezolid against both the standard and clinical S. aureus strains. This observation provides an impetus for the development of potential novel agents based on sy142 in the near future to combat MRSA and linezolid-resistant S. aureus.

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Antibacterial activity of LCB01-0062, a novel oxazolidinone

Cited by 7 publications

References 10 publications

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

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

Oxazolidinones as versatile scaffolds in medicinal chemistry

In Vitro Activity of Novel Oxazolidinone Analogs and 13 Conventional Antimicrobial Agents against Clinical Isolates of Staphylococcus aureus in Beijing, China

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