中文名 |
利福布丁 |
---|---|
英文名 |
Rifabutin |
中文别名 |
利福布汀 | 利福布汀(安莎霉素) | 4-N-异丁基螺哌啶利福霉素 S | 螺哌啶利福霉素S | 4-脱氧-3,4-[2-螺(N-异丁基-4-哌啶基)]-(1H)-咪唑并-(2,5-双氢)利福霉素S |
英文别名 |
更多 |
描述 |
Rifabutin (Ansamycin) 是半合成的安莎霉素抗生素,具有抗分枝杆菌特性。 |
||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
相关类别 |
|
||||||||||||
靶点 |
Antibacterial
|
||||||||||||
体外研究 |
利福布丁主要是用于治疗结核病的杀菌抗生素药物。它对细菌的作用是基于DNA依赖性RNA聚合酶阻断药物利福霉素S.,一种半合成衍生物。例如,它在高抗性分枝杆菌,革兰氏阳性菌(和一些对革兰氏阴性菌有效)中有效,但也对结核分枝杆菌,麻风杆菌和胞内分枝杆菌有效。利福布丁是一种抗生素;抗肿瘤。利福布汀干扰HSP-90分子伴侣,增强泛素化和蛋白质降解,并使细菌RNA聚合酶失活。 |
||||||||||||
溶解度 |
体外:
DMSO:≥100mg / mL(118.06 mM) * “≥”表示可溶,但饱和度未知。 体内:1。逐个添加每种溶剂:10%DMSO 40%PEG300 5%吐温-80 45%盐水溶解度:≥2.5mg/ mL(2.95mM);明确解决方案
|
||||||||||||
储备液 |
|
||||||||||||
存储 |
|
||||||||||||
运输 |
室温;可能会有所不同 |
||||||||||||
SMILES |
C[C@@]1(O2)O/C=C/[C@@H]([C@H]([C@H]([C@H](C)[C@H](O)[C@H](C)[C@H]([C@H](/C=C/C=C(C(NC(C3=O)=C4NC5(CCN(CC(C)C)CC5)N=C4C6=C3C(O)=C(C)C2=C6C1=O)=O)C)C)O)OC(C)=O)C)OC |
||||||||||||
参考文献 |
|
||||||||||||
相关活性 小分子 |
嘌呤霉素盐酸盐 | G-418 硫酸盐 | 衣霉素 | 潮霉素B | 盐霉素 | 阿维巴坦钠 | 硫酸新霉素 | 法硼巴坦 | 甲氧西林钠 | 利福平 | 甲硝唑 | 羧苄青霉素钠 | 头孢他啶 | Eravacycline dihydrochloride | 头孢噻肟钠 |
密度 | 1.3±0.1 g/cm3 |
---|---|
沸点 | 969.6±65.0 °C at 760 mmHg |
熔点 | 169-171?C |
分子式 | C46H62N4O11 |
分子量 | 847.005 |
闪点 | 540.2±34.3 °C |
精确质量 | 846.441528 |
PSA | 205.55000 |
LogP | 3.45 |
外观性状 | 红色-紫罗兰色结晶粉末 |
蒸汽压 | 0.0±0.3 mmHg at 25°C |
折射率 | 1.623 |
储存条件 | Amber Vial, -20°C Freezer, Under Inert Atmosphere |
水溶解性 | DMSO: >5mg/mL |
利福布汀毒性英文版
|
个人防护装备 |
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
---|---|
危险品运输编码 | NONH for all modes of transport |
RTECS号 | VJ6700000 |
海关编码 | 2941903000 |
【方法1】
以1,4-二氢利福霉素S为原料,经溴化,亚硝基取代,氢化,氨化,再和N-异丁基哌啶酮反应,即可得到利福布汀。
海关编码 | 2941903000 |
---|
Simple and accurate quantitative analysis of 20 anti-tuberculosis drugs in human plasma using liquid chromatography-electrospray ionization-tandem mass spectrometry. J. Pharm. Biomed. Anal. 102 , 9-16, (2014)
A simple and accurate liquid chromatography (LC)-tandem mass spectrometry (MS/MS) method for the quantitation of 20 anti-tuberculosis (anti-TB) drugs in human plasma, was developed as a tool for thera…
|
|
Different antibiotic susceptibility between antrum and corpus of the stomach, a possible reason for treatment failure of Helicobacter pylori infection. World J. Gastroenterol. 20(43) , 16245-51, (2014)
To assess whether antibiotic resistance varies between the antrum and corpus of the stomach of patients that are either Helicobacter pylori (H. pylori) therapy-naive or pre-treated.H. pylori strains w…
|
|
Genipin crosslinked ethyl cellulose-chitosan complex microspheres for anti-tuberculosis delivery. Colloids Surf. B Biointerfaces 103 , 530-7, (2013)
Genipin-crosslinked complex microspheres made of the combination of two polymers, ethyl cellulose and chitosan, were prepared by spray drying method. Rifabutin, an anti-tuberculosis agent was used as …
|
|
Rifabutin |
4-deoxo-3,4-[2-spiro(N-isobutyl-4-piperidyl)-2,5-dihydro-1H-imidazo]-rifamicin S |
Ansamycin |
RIFABUTINE |
Mycobutin |
lm427 |
Rifabatin |
antibioticlm427 |
1′,4-didehydro-1-desoxi-1,4-di-hydro-5′-(2-methyl-propyl)-1-oxo-rifamycin |
Ansatipine |
6,9-dihydro-5,17,19,21-tetrahydroxy-8,9-[2-spiro-(N-isobutyl-4-piperidyl)-2,5-dihydro-1H-imidazo]-23-methoxy-2,4,12,16,18,20,22-heptamethyl-6-oxo-2,7-epoxypentadeca-[1,11,13]-trienimine-2H-furo[2',3',7,8]nafto[1,2-d]imidazolo-2,4′-piperidine-5,10,26. (3H,9H)-trione-16-acetate |