Zoliflodacin (ETX0914;AZD0914) 是一种新型的螺旋嘧啶三酮,细菌DNA促旋酶/拓扑异构酶 抑制剂。Zoliflodacin 对革兰氏阳性和阴性生物具有有效的体外抗菌活性,对金黄色葡萄球菌的b>MIC90 值为0.25 μg/mL。
Description | Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus with the MIC90 of 0.25 μg/mL. | ||||||||||||||||
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IC50 & Target | MIC90: 0.25 μg/mL (S. aureus)[1] | ||||||||||||||||
In Vitro | Zoliflodacin has antibacterial activity against key Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzae, Neisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial species, including isolates with known resistance to fluoroquinolones. The antibacterial activity of Zoliflodacin is shown to be via inhibition of DNA biosynthesis and accumulation of double-strand cleavages; this mechanism of action differs from those of other marketed antibacterial compounds, including fluoroquinolones. Zoliflodacin stabilizes and arrests the cleaved covalent complex of gyrase with double-strand broken DNA under permissive conditions and thus blocks religation of the double-strand cleaved DNA to form fused circular DNA[1]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : 140 mg/mL (287.21 mM; Need ultrasonic) Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References |
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