Synthesis, Antibacterial Activities, Mode of Action and Acute Toxicity Studies of New Oxazolidinone-Fluoroquinolone Hybrids

To combat bacterial resistance, a series of new oxazolidinone-fluoroquinolone hybrids have been synthesized and characterized. All synthetic hybrids were preliminarily evaluated for their in vitro antibacterial activities against 6 standard strains and 3 clinical isolates. The majority of hybrids di...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2019-04, Vol.24 (8), p.1641
Main Authors: Liu, Lili, Shao, Liping, Li, Jing, Cui, Haifeng, Li, Bing, Zhou, Xuzheng, Lv, Pengyue, Zhang, Jiyu
Format: Article
Language:English
Subjects:
Acute toxicity
Antibacterial activity
Antibiotics
Antimicrobial agents
Bacteria
Clinical isolates
DNA biosynthesis
Drug resistance
Enzymes
Gram-negative bacteria
Gram-positive bacteria
Hybrids
Mode of action
Nosocomial infections
oxazolidinone-fluoroquinolone hybrids
Protein biosynthesis
Protein synthesis
Staphylococcus infections
Strains (organisms)
Streptococcus infections
synthesis
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Summary:To combat bacterial resistance, a series of new oxazolidinone-fluoroquinolone hybrids have been synthesized and characterized. All synthetic hybrids were preliminarily evaluated for their in vitro antibacterial activities against 6 standard strains and 3 clinical isolates. The majority of hybrids displayed excellent activities against Gram-positive bacteria, but limited activities against Gram-negative bacteria. Hybrids OBP-4 and OBP-5 were found to be the most promising compounds. Further, in vitro antibacterial activities, mode of action and acute toxicity in mice of hybrids OBP-4 and OBP-5 were investigated. Hybrids OBP-4 and OBP-5 exhibited potent activities against Gram-positive bacteria, including drug-resistant strains. Correspondingly, studies on the mode of action of hybrids OBP-4 and OBP-5 indicated a strong inhibitory activity on protein synthesis by binding the active site of 50S subunit, but a weak inhibitory action on DNA synthesis. In addition, LD values of hybrids OBP-4 and OBP-5 in the acute oral toxicity were larger than 2000 mg/kg, suggesting a good safety profile.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules24081641