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培氟沙星

培氟沙星用途

Pefloxacin是抗菌化合物,通过抑制DNA旋转酶来阻断DNA复制。

培氟沙星名称

[ CAS 号 ]:
70458-92-3

[ 中文名 ]:
培氟沙星

[ 英文名 ]:
Pefloxacin

[中文别名 ]:

培氟哌酸

[英文别名 ]:

MFCD01685696
PFLX
Abactal
Pefloxacine
Labocton
Silver Pefloxacin
Pefloxacin
Pefloxacino
Pefloxacin (USAN)
Pefloxacinum

培氟沙星生物活性

[ 描述 ]:

Pefloxacin是抗菌化合物,通过抑制DNA旋转酶来阻断DNA复制。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

天然产物 >> 生物碱

研究领域 >> 感染

[参考文献]

[1]. Drlica K, et al. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92.

[2]. Hussy P, et al. Effect of 4-quinolones and novobiocin on calf thymus DNA polymerase alpha primase complex, topoisomerases I and II, and growth of mammalian lymphoblasts. Antimicrob Agents Chemother. 1986 Jun;29(6):1073-8.

[相关活性小分子]

培氟沙星物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
529.1±50.0 °C at 760 mmHg

[ 分子式 ]:
C₁₇H₂₀FN₃O₃

[ 分子量 ]:
333.357

[ 闪点 ]:
273.8±30.1 °C

[ 精确质量 ]:
333.148865

[ PSA ]:
65.78000

[ LogP ]:
1.51

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.594

[ 储存条件 ]:
2-8℃

培氟沙星毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VB2002000

CHEMICAL NAME :: 3-Quinolinecarboxylic acid, 1,4-dihydro-1-ethyl-6-fluoro-7-(4-methyl-1-piperaziny l)-4-oxo-

CAS REGISTRY NUMBER :: 70458-92-3

BEILSTEIN REFERENCE NO. :: 0567618

LAST UPDATED :: 199806

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C17-H20-F-N3-O3

MOLECULAR WEIGHT :: 333.40

WISWESSER LINE NOTATION :: T66 BN VVJ B2 DVQ HF I- AT6N DNTJ D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1714 mg/kg/21W-I

TOXIC EFFECTS :: Peripheral Nerve and Sensation - paresthesis Peripheral Nerve and Sensation - structural change in nerve or sheath

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 343 mg/kg/30D-I

TOXIC EFFECTS :: Musculoskeletal - joints Musculoskeletal - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 16 mg/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - muscle contraction or spasticity

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 225 mg/kg

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

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >50 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 :: 7500 mg/kg/30D-C

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30 gm/kg

SEX/DURATION :: male 30 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

MUTATION DATA

TYPE OF TEST :: Unscheduled DNA synthesis

TEST SYSTEM :: Rodent - rat Liver

DOSE/DURATION :: 780 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 221,263,1989

培氟沙星安全信息

[ 危害码 (欧洲) ]:
N

[ 风险声明 (欧洲) ]:
R51/53:Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment .

[ 安全声明 (欧洲) ]:
S61

[ 危险品运输编码 ]:
UN 3082

[ RTECS号 ]:
WM6250000

培氟沙星合成路线

详细合成路线

培氟沙星上下游产品

培氟沙星上游产品

培氟沙星下游产品

培氟沙星制备

1.诺氟沙星为原料，经甲基化而得产品。

2.从诺氟沙星中的中间体硼螯合物开始制备。该硼螫合物、乙腈、N- 甲基哌嗪和三乙胺混合，室温反应后再回流。蒸除溶剂，加水，浓盐酸调至Ph=3后再回流。加入活性炭脱色，过滤。滤液碱化至Ph=11，再加活性炭脱色，过滤，用30%醋酸中和至Ph=6.7-7.2，冰箱中过夜。过滤，水洗，干燥得类白色的培氟沙星，收率82%，熔点270-272℃。培氟沙星溶入无水乙醇中，在60～70℃下滴加甲磺酸，反应。冷至15℃，过滤析出的结晶，用10倍乙醇重结晶，得甲磺酸培氟沙星，收率88.5%。

3.也可硼螯合物、N-甲基哌嗪和三乙胺一起回流。再碱性水解，酸化至Ph=7.2，得培氟沙星；将其加入甲磺酸的水溶液中，反应得到的粗品用85%乙醇重结晶，得甲磺酸培氟沙星，收率79.4%，熔点284℃。