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氧氟沙星

氧氟沙星用途

Ofloxacin是氟喹诺酮类抗生素,可抑制细菌DNA旋转酶。
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氧氟沙星名称

[ CAS 号 ]:
82419-36-1

[ 中文名 ]:
氧氟沙星

[ 英文名 ]:
Ofloxacin

[中文别名 ]:

[英文别名 ]:

氧氟沙星生物活性

[ 描述 ]:

Ofloxacin是氟喹诺酮类抗生素,可抑制细菌DNA旋转酶。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌
研究领域 >> 感染

[参考文献]

[1]. Todd PA, et al. Ofloxacin. A reappraisal of its antimicrobial activity, pharmacology and therapeutic use. Drugs. 1991 Nov;42(5):825-76.

[2]. Smith JT, et al. Ofloxacin, a bactericidal antibacterial. Chemotherapy. 1991;37 Suppl 1:2-13.

[3]. Olcay E, et al. Oral toxicity of pefloxacin, norfloxacin, ofloxacin and ciprofloxacin: comparison of biomechanical and histopathological effects on Achilles tendon in rats. J Toxicol Sci. 2011 Jun;36(3):339-45.


[相关活性小分子]

嘌呤霉素二盐酸盐 | 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 | 盐酸依拉环素 | 头孢噻肟钠

氧氟沙星物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
571.5±50.0 °C at 760 mmHg

[ 熔点 ]:
270-2750C

[ 分子式 ]:
C18H20FN3O4

[ 分子量 ]:
361.367

[ 闪点 ]:
299.4±30.1 °C

[ 精确质量 ]:
361.143799

[ PSA ]:
75.01000

[ LogP ]:
0.84

[ 外观性状 ]:
灰白色固体

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.670

[ 储存条件 ]:
2-8°C

氧氟沙星MSDS

详细MSDS(安全技术说明书)

氧氟沙星毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UU8815500
CHEMICAL NAME :
7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 2,3-dihydro-9-fluoro-3-methyl-10- (4-methyl-1-piperazinyl)-7-oxo-, (+-)-
CAS REGISTRY NUMBER :
82419-36-1
LAST UPDATED :
199806
DATA ITEMS CITED :
28
MOLECULAR FORMULA :
C18-H20-F-N3-O4
MOLECULAR WEIGHT :
361.41

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
17 mg/kg/3D-I
TOXIC EFFECTS :
Behavioral - excitement Blood - changes in cell count (unspecified) Skin and Appendages - dermatitis, allergic (after systemic exposure)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
24 mg/kg/3D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis Behavioral - irritability
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
51428 ug/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - body temperature increase
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3590 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
7070 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
273 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - coma Lungs, Thorax, or Respiration - respiratory depression
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3266 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
805 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
7690 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 :
208 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - coma Lungs, Thorax, or Respiration - respiratory depression
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>600 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>200 mg/kg
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - hypermotility, diarrhea
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>70 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 :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
7560 mg/kg/4W-I
TOXIC EFFECTS :
Behavioral - fluid intake Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
5600 mg/kg/4W-I
TOXIC EFFECTS :
Gastrointestinal - other changes 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 :
990 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1620 mg/kg
SEX/DURATION :
female 9-10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
8910 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2080 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death

MUTATION DATA

TYPE OF TEST :
DNA inhibition
TEST SYSTEM :
Mammal - domestic Cells - not otherwise specified
DOSE/DURATION :
27 mg/L
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 34,1955,1990
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氧氟沙星安全信息

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

[ 危害码 (欧洲) ]:
Xn, Xi

[ 风险声明 (欧洲) ]:
22-42/43-68-36/37/38

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S24/25-S22

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UU8815550

[ 海关编码 ]:
2934999090

氧氟沙星合成路线

详细合成路线

氧氟沙星上下游产品

氧氟沙星上游产品

氧氟沙星下游产品

氧氟沙星制备

方法1：以2，3，4-三氟硝基苯为起始原料，经选择性碱水解、醚化、还原、与C2H5OCH=C(COOEt)2或(CH3)2NCH=C(COOEt)2缩合、环合、水解，与乙酸硼作用后，再引入N-甲基哌嗪而得产品。

方法2：以邻苯二甲酰亚胺衍生物为原料，经氟化生成四氟邻苯二甲酰亚胺，水解、脱羧生成2，3，4，5-四氟苯甲酸，再氯化、酰化、脱羧生成2，3，4，5-四氟苯甲酰乙酸乙酯，接着先和原甲酸三乙酯、后和2-氨基丙醇反应，再环合生成吡啶并[1，2，3-de][1，4]苯并嘿嗪衍生物，最后和哌嗪反应生成氧氟沙星。

方法3：上述得到的四氟苯甲酰乙酸乙酯，先和甲基哌嗪反应，引入哌嗪基后，再引入侧链后环合，然后水解得氧氟沙星。在氧氟沙星的制备中，哌嗪基的引入是一研究热点。越后引入，对其收率影响越大。该方法先把哌嗪引入，其引入收率可达88%。但在环合时，必须用强碱，如氢化钠，才能进行环合。

4.以2,3,4-三氟硝基苯为原料，经选择性碱水解、醚化、还原、缩合、环合、水解，与乙酸硼作用后，再引入犖甲基哌嗪而得产品。或者以邻苯二甲酰亚胺衍生物为原料，经氟化生成四氟邻苯二甲酰亚胺，经水解、脱羧生成2,3,4,5,-四氟苯甲酸，再氯化、酰化、脱羧生成2,3,4,5,-四氟苯甲酰乙酸乙酯。然后和原甲酸三乙酯、再和2-氨基丙醇反应，最后和哌嗪反应生成氧氟沙星。也可以将上述得到的2,3,4,5,-四氟苯甲酰乙酸乙酯，先和甲基哌嗪反应，引入哌嗪基后，再引入侧链后环合，然后水解得氧氟沙星。
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氧氟沙星海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氧氟沙星文献

Targeting the gyrase of Plasmodium falciparum with topoisomerase poisons.

Biochem. Pharmacol. 95 , 227-37, (2015)

Drug-resistant malaria poses a major public health problem throughout the world and the need for new antimalarial drugs is growing. The apicoplast, a chloroplast-like organelle essential for malaria p...

Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.

Antimicrob. Agents Chemother. 52 , 3052-60, (2008)

Active efflux of antimicrobial agents is one of the most important adapted strategies that bacteria use to defend against antimicrobial factors that are present in their environment. The NorM protein ...

Evaluation of Antioxidant and Antibacterial Potentials of Nigella sativa L. Suspension Cultures under Elicitation.

Biomed Res. Int. 2015 , 708691, (2015)

Nigella sativa L. (family Ranunculaceae) is an annual herb of immense medicinal properties because of its major active components (i.e., thymoquinone (TQ), thymohydroquinone (THQ), and thymol (THY)). ...


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推荐生产厂家/供应商：

公司名：上海吉至生化科技有限公司

区域：上海市奉贤区

价格：
￥118.0/5g ￥348.0/25g ￥108.0/100mg

联系人：刘佳

产品详情：氧氟沙星

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Ofloxacin

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥95.0/1g ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：李先生

产品详情：氧氟沙星

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥466.9/100mg ￥39.9/1g ￥101.9/5g ￥205.9/1ml

联系人：阿拉丁李高志

产品详情：Ofloxacin

公司名：上海创赛科技有限公司

区域：上海市嘉定区

价格：
￥41.0/1g ￥101.0/5g ￥289.0/25g ￥935.0/100g

联系人：夏言

产品详情：[Perfemiker]氧氟沙星,98%

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【氧氟沙星】化源网提供氧氟沙星CAS号82419-36-1，氧氟沙星MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询氧氟沙星上化源网，专业又轻松。>>电脑版：氧氟沙星

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