790703-49-0Relevant articles and documents
Synthesis, antibacterial activities, mode of action and acute toxicity studies of new oxazolidinone-fluoroquinolone hybrids
Liu, Lili,Shao, Liping,Li, Jing,Cui, Haifeng,Li, Bing,Zhou, Xuzheng,Lv, Pengyue,Zhang, Jiyu
, (2019/05/01)
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, LD50 values of hybrids OBP-4 and OBP-5 in the acute oral toxicity were larger than 2000 mg/kg, suggesting a good safety profile.
Preparation method of Cadazolid key intermediate
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Paragraph 0040-0053, (2018/06/04)
The invention discloses a preparation method of a Cadazolid key intermediate. The preparation method comprises following steps: reacting a compound represented by the formula (4) with a non-nucleophilic strong base, reacting the reaction product with (R)-
INTERMEDIATE PRODUCTS FOR PRODUCING OXAZOLIDINONE-QUINOLONE HYBRIDS
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Page/Page column 24, (2008/06/13)
The invention relates to intermediate products (ZP) for a novel and efficient synthesis of compounds, wherein the pharmacophores of quinolone and oxazolidinone are linked together by means of a chemically stable linker.