189279-58-1
189279-58-1 結(jié)構(gòu)式
基本信息
地拉沙星游離酸
ABT-492圖片
ABT-492品牌
1-(6-氨基-3
化合物DELAFLOXACIN
5-二氟-2-吡啶基)-8-氯-6-氟-1
4-二氫-7-(3-羥基-1-氮雜環(huán)丁基)-4-氧代-3-喹啉羧酸
1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-7-(3-羥基-1-氮雜環(huán)丁基)-4-氧代-1,4-二氫喹啉-3-羧酸
1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-1,4-二氫-7-(3-羥基-1-氮雜環(huán)丁基)-4-氧代-3-喹啉羧酸
CS-711
RX-3341
ABT-492
CS-2335
Delafloxacin
Delafloxacinum
ABT492/ABT-492
ABT-492(WQ-3034)
ABT-492/Delafloxacin
物理化學(xué)性質(zhì)
常見問題列表
德拉沙星是一種有效的抗肺炎鏈球菌和多種病原體的試劑和廣譜陰離子氟喹諾酮。
1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-1,4-二氫-7-(3-羥基-1-氮雜環(huán)丁基)-4-氧代-3-喹啉羧酸是有機(jī)合成中間體和醫(yī)藥中間體，可用于實(shí)驗(yàn)室研發(fā)合成過程和化工生物研發(fā)過程中。
德拉沙星是一種氟喹諾酮類抗菌藥適用于成年為被指定的一種細(xì)菌所致的急性細(xì)菌性皮膚和皮膚結(jié)構(gòu)感染(ABSSSI)的治療。
Antibiotic
德拉沙星最常見不良反應(yīng)(發(fā)生率 ≥ 2%)是惡心，腹瀉，頭痛，轉(zhuǎn)氨酶升高和嘔吐。
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. |