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利福布汀

利福布汀

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?利福布汀名称


















中文名

利福布丁
英文名

Rifabutin
中文别名


利福布汀




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利福布汀(安莎霉素)




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4-N-异丁基螺哌啶利福霉素 S




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螺哌啶利福霉素S




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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





?利福布汀生物活性
















































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

1 mM 1.1806 mL 5.9032 mL 11.8064 mL
5 mM 0.2361 mL 1.1806 mL 2.3613 mL
10 mM 0.1181 mL 0.5903 mL 1.1806 mL


存储

粉末 -20℃下 3年
4℃下 2年
在溶剂中 -80℃下 6个月
-20℃下 1个月


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

[1]. Review Article: Rifabutin in the Treatment of Refractory Helicobacter pylori Infection J. P. Gisbert, X. Calvet Issue Alimentary Pharmacology & Therapeutics Volume 35, Issue 2, pages 209-221, January 2012

[2]. Vourvahis M, Davis J, Wang R, Layton G, Choo HW, Chong CL, Tawadrous M.Effect of rifampin and rifabutin on the pharmacokinetics of lersivirine and effect of lersivirine on the pharmacokinetics of rifabutin and 25-o-desacetyl-rifabutin in healthy subjects.Antimicrob Agents Chemother. 2012 Aug;56(8):4303-9.

[3]. Gisbert JP, Castro-Fernandez M, Perez-Aisa A, Cosme A, Molina-Infante J, Rodrigo L, Modolell I, Cabriada JL, Gisbert JL, Lamas E, Marcos E, Calvet X.Fourth-line rescue therapy with rifabutin in patients with three Helicobacter pylori eradication failures.Aliment Pharmacol Ther. 2012 Apr;35(8):941-7. doi: 10.1111/j.1365-2036.2012.05053.x.

[4]. Gisbert JP, Calvet X.Review article: rifabutin in the treatment of refractory Helicobacter pylori infection.Aliment Pharmacol Ther. 2012 Jan;35(2):209-21. doi: 10.1111/j.1365-2036.2011.04937.x.

[5]. Horne DJ, Spitters C, Narita M.Experience with rifabutin replacing rifampin in the treatment of tuberculosis.Int J Tuberc Lung Dis. 2011 Nov;15(11):1485-9, i.


相关活性
小分子




嘌呤霉素盐酸盐



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G-418 硫酸盐



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衣霉素



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潮霉素B



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盐霉素



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阿维巴坦钠



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硫酸新霉素



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法硼巴坦



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甲氧西林钠



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利福平



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甲硝唑



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羧苄青霉素钠



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头孢他啶



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Eravacycline dihydrochloride



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头孢噻肟钠






?利福布汀物理化学性质













































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





?利福布汀毒性和生态




利福布汀毒性英文版






?利福布汀安全信息






















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








?利福布汀制备



【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。







?利福布汀海关









海关编码 2941903000








?利福布汀文献62

更多文献














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 …









?利福布汀英文别名










































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








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