水合加替沙星
水合加替沙星 性质
| 沸点 | 684℃ |
|---|---|
| RTECS号 | VB1983600 |
| 储存条件 | Keep in dark place,Inert atmosphere,2-8°C |
| 溶解度 | 溶于 1N NaOH，浓度为 10mg/ml |
| 形态 | powder |
| 颜色 | white to beige |
| BRN | 14390028 |
| InChI | InChI=1S/C19H22FN3O4.H2O/c1-10-8-22(6-5-21-10)16-14(20)7-12-15(18(16)27-2)23(11-3-4-11)9-13(17(12)24)19(25)26;/h7,9-11,21H,3-6,8H2,1-2H3,(H,25,26);1H2 |
| InChIKey | IJOOSVJZBQQMBV-UHFFFAOYSA-N |
| SMILES | O(C1C(N2CCNC(C)C2)=C(F)C=C2C(=O)C(C(=O)O)=CN(C3CC3)C=12)C.O |
水合加替沙星 用途与合成方法
水合加替沙星是一种口服氟喹诺酮类广谱抗生素，通过抑制细菌的DNA旋转酶和拓扑异构酶IV发挥作用，并增强了对革兰氏阳性菌及厌氧菌的抗菌活性。
水合加替沙星可用于治疗眼部感染，且未见引起光毒性反应。
水合加替沙星(AM-1155 sesquihydrate) 是一种有效的氟喹诺酮类抗生素 (antibiotic)，具有广谱抗菌活性。其可抑制细菌 II 型拓扑异构酶 (type II topoisomerases) (IC50=13.8 μg/ml; 金黄色葡萄球菌拓扑异构酶 IV) 和大肠杆菌 DNA 解旋酶 (IC50=0.109 μg/ml)。其在动物模型中，可用于细菌性结膜炎的研究。
|
Topoisomerase II 36.7 μM (IC 50 ) |
Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC 50 values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively.Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with MIC values of 0.05 μg/ml, 0.0063 μg/ml, and 122 μg/ml, respectively.Gatifloxacin sesquihydrate exhibits antibacterial activities for wild-type strains (MS5935, MS5952, MR5867 and MR6009) the first-, second-, third-, and fourth-step mutants with MIC values of 0.05 to 0.10 μg/ml, 0.20 μg/ml, 1.56 to 3.13 μg/ml, 1.56 to 6.25 μg/ml, and 50 to 200 μg/ml, respectively. Gatifloxacin sesquihydrate displays the most potent activity against the second- and third-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS5935.Gatifloxacin sesquihydrate has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml).Gatifloxacin sesquihydrate (20-100 μM; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to be reduced to 50.1% and 44.7% at Day 3 by 20 μM and 100 μM Gatifloxacin sesquihydrate, respectively.
Gatifloxacin sesquihydrate (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis .
| Animal Model: | Female BALB/c mice with Nocardia brasiliensis in the right hind footpad |
| Dosage: | 100 mg/kg |
| Administration: | Subcutaneous injection; 3 times a day; 30 days |
| Result: | Reduced the production of lesions in mice. |
安全信息
| 危险品标志 | Xn |
|---|---|
| 危险类别码 | 20/21/22 |
| 安全说明 | 36/37 |
| WGK Germany | 1 |
| 存储类别 | 11 - 可燃固体 |
| 危险性类别 | 急性毒性 类别4 经皮 急性毒性 类别4 吸入 急性毒性 类别4 经口 |
