151213-16-0
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- CAS号:
- 151213-16-0
- 英文名:
- BAY-Y 3118
- 英文别名:
- BAY Y 3118,BAYY 3118;3-Quinolinecarboxylic acid, 8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-
- 中文名:
- 151213-16-0
- 中文别名:
- 化合物 T10478
- CBNumber:
- CB53339610
- 分子式:
- C20H21ClFN3O3
- 分子量:
- 405.85
- MOL File:
- 151213-16-0.mol
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151213-16-0化学性质
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沸点:
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627.2±55.0 °C(Predicted)
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密度:
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1.486±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Solid
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酸度系数(pKa):
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6.40±0.50(Predicted)
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颜色:
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White to light yellow
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151213-16-0性质、用途与生产工艺
BAY-Y 3118是一种具有抗菌活性的新氯氟喹诺酮。
BAY-Y 3118 is potent against
Haemophilhs influenzae, Moraxela catarrhalis, Acinetobacter baumannii, Xanthomonas maltophiia, gram-positive cocci
, and anaerobes; MICs for 50%o of the strains (MIC
50
s) and MIC
90
s are ≤0.015 and ≤0.015, ≤0.015 and ≤0.015, 0.03 and 2, 0.25 and 0.5, 0.06 and 1, and 0.12 and 0.25 μg/mL, respectively. The cellular concentration-to-extracellular concentration ratio of BAY-Y 3118 is higher than 6.3 at extracellular concentrations ranging from 2 to 100 mg/L. The uptake of BAY-Y 3118 is rapid, reversible and nonsaturable. The intracellular penetration of BAY-Y 3118 is significantly affected by environmental temperature and cell viability. BAY-Y 3118 reaches high intracellular concentrations within human polymorphonuclear leukocytes (PMNs) and remains active intracellularly. All strains of
L. monocytogenes
and other
Listeria
spp. are highly susceptible; the MICs for these organisms ranges from 0.062 to 0.25 μg/mL. BAY-Y 3118 is rapidly bactericidal
in vitro
, with a postantibiotic effect occurring for 3 h after removal of the antibiotic.
L. monocytogenes
is eliminated from infected L929 cells treated with BAY-Y 3118, suggesting a bactericidal effect on the listeriae in these cells.
Immunocompetent mice are rapidly cured by treatment with 4 mg every 12 h. Concomitantly, the levels of interleukin 6 and gamma interferon in mouse sera decline rapidly. In immunocompetent mice, treatment with 2 mg of BAY-Y 3118 every 12 h results in a greater initial reduction in the listerial counts in the organs than treatment with 2 mg of ampicillin every 12 h. BAY-Y 3118 completely eliminates
L. monocytogenes
from the livers and spleens of chronically infected nude mice.
151213-16-0
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下游产品
151213-16-0, 151213-16-0 相关搜索:
- 化合物 T10478
- 151213-16-0
- 3-Quinolinecarboxylic acid, 8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-
- BAY Y 3118,BAYY 3118