- 英文名称
- Delafloxacin
- 分子式
- C18H12ClF3N4O4
- 分子量
- 440.76
- 中文别名
- 地拉沙星游离酸; 德拉沙星API; 1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-1,4-二氢-7-(3-羟基-1-氮杂环丁基)-4-氧代-3-喹啉羧酸; ABT-492; Delafloxacinum; WQ3034; WQ-3034; RX-3341; Baxdela; 1-(6-Amino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-3-quinolinecarboxylic acid; 3-Quinolinecarboxylic acid, 1-(6-aMino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-; 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxoquinoline-3-carboxylic acid; 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboxylic acid; 1-(6-Amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid; 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid; Delafloxacin (USAN)
- 用途
- - 德拉沙星是一种有效的抗肺炎链球菌和多种病原体的试剂和广谱阴离子氟喹诺酮。
- 生物活性
Delafloxacin (ABT-492, RX-3341, WQ-3034)是一种氟喹诺酮，抗155需氧和171厌氧病原体。
- 适应症
德拉沙星是一种氟喹诺酮类抗菌药适用于成年为被指定的一种细菌所致的急性细菌性皮肤和皮肤结构感染(ABSSSI)的治疗。
- 靶点
Antibiotic
- 副作用
德拉沙星最常见不良反应(发生率 ≥ 2%)是恶心，腹泻，头痛，转氨酶升高和呕吐。
- 体内研究
Delafloxacin (the total daily doses vary from 0.156 to 640 mg/kg/24 h, subcutaneous injection) is highly effective against
S. aureus
. Against all four strains are observed a decrease of 1.5 to 2.2 log
10
CFU in organism burden from untreated controls at even the lowest dose studied, and for two strains (MW2 and R2527) there is net bactericidal activity at the lowest dose. At the maximal doses studied, there is a >4-log
10
kill from initial burden for all
S. aureus
strains.
Delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) has moderate terminal elimination half-life (t
1/2
=0.68 h, 0.79 h, 0.69 h and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively).
Animal Model:
Mice with a neutropenic murine lung infection model (four
S. aureus
, four
S. pneumoniae
, and four
K. pneumoniae
strains)
Dosage:
The total daily doses vary from 0.156 to 640 mg/kg/24 h
Administration:
0.03 to 160 mg/kg are administered every 6 h (q6h) to infected mice by subcutaneous injection
Result:
Inhibited
S. aureus
strains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively.
Inhibited
S. pneumoniae
strains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively.
Inhibited
K. pneumonia
strains ATCC 43816, 4105, 4110, and 81-1260A with MICs of 0.06, 1, 0.5, and 0.06 mg/L, respectively.
Animal Model:
Neutropenic mice
Dosage:
2.5, 10, 40, and 160 mg/kg; 0.2 mL
Administration:
Subcutaneous injection; 24 h
Result:
The maximum drug concentrations (C
max
) concentrations ranged from 2 to 71 mg/L. AUC
0-∞
values ranged from 2.8 to 152 mg•h/L and were linear across the 2.5- to 160-mg dosing range. The elimination half-life (t
1/2
) ranged from 0.7 to 1 h.
