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氟罗沙星

氟罗沙星用途

Fleroxacin是广谱的氟喹诺酮类抗菌素。

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氟罗沙星名称

[ CAS 号 ]:
79660-72-3

[ 中文名 ]:
氟罗沙星

[ 英文名 ]:
Fleroxacin

[中文别名 ]:

[英文别名 ]:

Fleroxacin
MEGALONE
ro23-6240/000
Megalocin
AM-833
Quinodis
hyl-1-piperazinyl)-4-oxo
MFCD00864880
RO-23-6240

氟罗沙星生物活性

[ 描述 ]:

Fleroxacin是广谱的氟喹诺酮类抗菌素。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[参考文献]

[1]. Weidekamm, E., et al., Single- and multiple-dose pharmacokinetics of fleroxacin, a trifluorinated quinolone, in humans. Antimicrob Agents Chemother, 1987. 31(12): p. 1909-14.

[2]. MacDonald, K.S., et al., Evaluation of fleroxacin (RO 23-6240) as single-oral-dose therapy of culture-proven chancroid in Nairobi, Kenya. Antimicrob Agents Chemother, 1989. 33(5): p. 612-4.

[3]. Rubinstein, E., History of quinolones and their side effects. Chemotherapy, 2001. 47 Suppl 3: p. 3-8; discussion 44-8.

[相关活性小分子]

氟罗沙星物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
535.3±50.0 °C at 760 mmHg

[ 熔点 ]:
264-266°C

[ 分子式 ]:
C₁₇H₁₈F₃N₃O₃

[ 分子量 ]:
369.338

[ 闪点 ]:
277.6±30.1 °C

[ 精确质量 ]:
369.130035

[ PSA ]:
65.78000

[ LogP ]:
1.72

[ 外观性状 ]:
白色针状晶体

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.568

[ 储存条件 ]:
2-8°C

氟罗沙星MSDS

详细MSDS(安全技术说明书)

氟罗沙星毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VB1999050

CHEMICAL NAME :: 3-Quinolinecarboxylic acid, 1,4-dihydro-6,8-difluoro-1-(2-fluoroethyl)-7-(4-methy l-1- piperazinyl)-4-oxo-

CAS REGISTRY NUMBER :: 79660-72-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C17-H18-F3-N3-O3

MOLECULAR WEIGHT :: 369.38

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 20405 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 21730 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Musculoskeletal - joints

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 109 gm/kg/13W-I

TOXIC EFFECTS :: Musculoskeletal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 4550 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Musculoskeletal - joints Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 26 gm/kg

SEX/DURATION :: male 61 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1300 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion Reproductive - Specific Developmental Abnormalities - musculoskeletal system

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Bacteria - Bacillus subtilis

DOSE/DURATION :: 400 ng/disk

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 38(Suppl 2),252,1990

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氟罗沙星安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
VB1999050

[ 海关编码 ]:
2933990090

氟罗沙星上下游产品

氟罗沙星上游产品

氟罗沙星下游产品

氟罗沙星制备

1. 2,3,4-三氟苯胺和乙氧基亚甲基丙二酸二乙酯,在150℃反应，并蒸去生成的乙醇。然后加入十六烷，在200~220℃下进行环合，生成6,7,8-三氟-4-氧代-3-喹啉羧酸乙酯(I)，收率90％。化合物(Ⅰ)和无水碳酸钾溶于二甲基甲酰胺，在室温下缓慢滴加氟溴乙烷。滴毕，升至60~70℃反应，得化合物(Ⅱ)，收率79％。硼酸和乙酸酐在室温下搅拌后，加入化合物(Ⅱ)，在105~110℃下反应。得化合物(Ⅲ)，收率80％。化合物(Ⅲ)和N-甲基哌嗪溶于二甲亚砜，于80~90℃下反应，得化合物(Ⅳ)，收率89.1％。化合物(Ⅳ)、95％乙醇和三乙胺，一起回流，水解得氟罗沙星，收率90％。总收率40％。

2. 6,7,8-三氟-1-(2-氟乙基)-1,4-二氢-4-氧代-3-喹啉酸乙酯的制备
在反应瓶中加入6,7,8-三氟-1,4-二氢-4-氧代-3-喹啉羧酸乙酯60g(0.22mol)、无水碳酸钾50g(0.36mol)、碘化钾18g(0.11mol)和DMF240ml,搅拌加热至90ºC,滴加1-溴-2-氟乙烷 42g(0.33mol),滴毕,保温搅拌反应10h.减压回收DMF冷至室温#加入水适量,过滤,滤饼用水洗,乙醇洗,得类白色固体6,7,8-三氟-1-(2-氟乙基)-1,4-二氢-4-氧代-3-喹啉酸乙酯64.5g,收率92.5%.

3. 6,8-二氟-1-(2-氟乙基)-1,4-二氢-7-(4-甲基-1-哌嗪基)-4-氧代-3-喹啉羧酸乙酯的制备
在反应瓶中加入6,7,8-三氟-1-(2-氟乙基)-1,4-二氢-4-氧代-3-喹啉酸乙酯64g(0.2mol)和N-甲基哌嗪
160g(1.6mol),搅拌加热至110ºC,搅拌反应6h.减压回收N-甲基哌嗪(约110g)冷却,加适量水稀释,析
出固体过滤,水洗滤饼,得类白色固体6,8-二氟-1-(2-氟乙基)-1,4-二氢-7-(4-甲基-1-哌嗪基)-4-氧代-3-喹啉羧酸乙酯70.5g,收率88.8%.(该步反应中加适量K2CO3对反应有促反应完全作用.)

4. 盐酸氟罗沙星的合成
在反应瓶中加入6,8-二氟-1-(2-氟乙基)-1,4-二氢-7-(4-甲基-1-哌嗪基)-4-氧代-3-喹啉羧酸乙酯60g(0.15mol)与3%NaOH溶液600ml,搅拌加热至85ºC,保温搅拌反应1h.过滤,滤液用乙酸调至pH7.2,降温,过滤,滤饼依次用适量水、乙醇洗,干燥得白色固体45.5g,收率82.2%.

取白色固体36.9g(0.1,ol)、370ml乙醇,搅拌混合,加入18%盐酸水溶液,加热回流4h.冷却析晶,过滤,滤液依次用冷乙醇洗,乙醚洗,抽干,用水重结晶得盐酸氟罗沙星38.0g,收率93.6%.

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氟罗沙星海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氟罗沙星文献

Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.

Bioorg. Med. Chem. 17 , 6983-92, (2009)

Computational modeling continues to play an important role in novel therapeutics discovery and development. In this study, we have investigated the use of in silico approaches to develop inhibitors of...

QSAR-based permeability model for drug-like compounds.

Bioorg. Med. Chem. 19 , 2615-24, (2011)

A QSAR model was developed for predicting intestinal drug permeability, one of the most important parameters when evaluating compounds in drug discovery projects. First, a set of relevant properties f...

Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.

Drug Metab. Dispos. 36 , 1385-405, (2008)

We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic ...

更多文献

氟罗沙星

氟罗沙星用途

氟罗沙星名称

氟罗沙星生物活性

氟罗沙星物理化学性质

氟罗沙星MSDS

详细MSDS(安全技术说明书)

氟罗沙星毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

氟罗沙星安全信息

氟罗沙星上下游产品

氟罗沙星上游产品

氟罗沙星下游产品

氟罗沙星制备

氟罗沙星海关

氟罗沙星文献

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