ABT-492
| 中文名称 | ABT-492 |
|---|---|
| 中文同义词 | 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;地拉沙星游离酸;ABT-492品牌;ABT-492图片;4-二氢-7-(3-羟基-1-氮杂环丁基)-4-氧代-3-喹啉羧酸;5-二氟-2-吡啶基)-8-氯-6-氟-1;1-(6-氨基-3 |
| 英文名称 | ABT-492 |
| 英文同义词 | ABT-492;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;Delafloxacinum;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-;WQ3034;ABT-492(WQ-3034);ABT492/ABT-492;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 |
| CAS号 | 189279-58-1 |
| 分子式 | C18H12ClF3N4O4 |
| 分子量 | 440.76 |
| EINECS号 | |
| 相关类别 | 信号转导通路激酶抑制剂;抑制剂;微生物Microbiology;中间体;原料药;医药化工原料-医药原料药;API;医药原料药 |
| Mol文件 | 189279-58-1.mol |
| 结构式 |  |
ABT-492 性质
| 熔点 | 238-241℃ |
|---|---|
| 沸点 | 698.5±55.0 °C(Predicted) |
| 密度 | 1.796 |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO（轻微）、甲醇（非常轻微、加热、超声处理） |
| 酸度系数(pKa) | 5.49±0.50(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| CAS 数据库 | 189279-58-1 |
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 是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。
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-喹啉羧酸是原料药德拉沙星的杂质，可用于实验室研发过程和化工医药合成过程中，德拉沙星是一种广谱氟喹诺酮类抗生素。德拉沙星具有广泛的活性，对耐药性的金黄色葡萄球菌，肺炎链球菌和肺炎克雷伯菌都有效。
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-喹啉羧酸是有机合成中间体和医药中间体，可用于实验室研发合成过程和化工生物研发过程中。
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。Antibiotic
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. |