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美西林

美西林用途

Mecillinam (Amdinocillin) 是一种β 内酰胺类抗生素,具有广谱的抗革兰氏阴性菌的活性。

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美西林名称

[ CAS 号 ]:
32887-01-7

[ 中文名 ]:
美西林

[ 英文名 ]:
Mecillinam

[中文别名 ]:

氮卓脒青霉素

[英文别名 ]:

Amdinocillin
Mecillinam
EINECS 251-277-1
MFCD00056869

美西林生物活性

[ 描述 ]:

Mecillinam (Amdinocillin) 是一种β 内酰胺类抗生素,具有广谱的抗革兰氏阴性菌的活性。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[体内研究]

美西林(Amdinocillin,400 mg/kg)对高剂量(400 mg/kg体重/d)的导管相关感染有效[1]。动物模型：美西林(Amdinocillin,400mg/kg)对高剂量(400mg/kg体重/d)的导管相关性感染有效[1]。剂量：每公斤50、100、200和400毫克。给药：每天静脉注射,分四次,持续72小时。结果：大剂量400mg/kg具有显著的活性。

[参考文献]

[1]. M E Olson, et al. Amdinocillin Treatment of Catheter-Associated Bacteriuria in Rabbits. J Infect Dis. 1989 Jun;159(6):1065-72.

美西林物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
581.0±60.0 °C at 760 mmHg

[ 熔点 ]:
156°C

[ 分子式 ]:
C₁₅H₂₃N₃O₃S

[ 分子量 ]:
439.569

[ 闪点 ]:
305.2±32.9 °C

[ 精确质量 ]:
439.214081

[ PSA ]:
98.51000

[ LogP ]:
2.97

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.604

[ 储存条件 ]:
Store at?0-5°C

美西林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XI0185000

CHEMICAL NAME :: 4-Thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((hexahydro-1H-azepin-1-yl)methylene) amino)-3,3-dimethyl-7-oxo-, (+)-

CAS REGISTRY NUMBER :: 32887-01-7

LAST UPDATED :: 199512

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C15-H23-N3-O3-S

MOLECULAR WEIGHT :: 325.47

WISWESSER LINE NOTATION :: T45 ANV ESTJ F1 F1 GVQ CNU1- AT7NTJ

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 :: >10 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 9,91,1980

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 9,91,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1500 mg/kg

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

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 16,191,1980

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >20 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 9,91,1980

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3500 mg/kg

TOXIC EFFECTS :: Blood - other changes

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 9,91,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1200 mg/kg

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

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 16,191,1980 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 130 gm/kg/26W-I

TOXIC EFFECTS :: Blood - normocytic anemia Liver - changes in liver weight Related to Chronic Data - changes in testicular weight

REFERENCE :: EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 9,91,1980

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美西林安全信息

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

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26

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

[ RTECS号 ]:
XI0185000

美西林合成路线

详细合成路线

美西林上下游产品

美西林上游产品

美西林下游产品

美西林制备

方法1：氮杂革和三氯乙醛作用，在氮上引入甲酰基，在硫酸二甲酯作用下形成缩醛，和6-APA反应使6-APA上6位上的氨基形成Schiff’S碱，即为美西林。
方法2：6-APA和六甲基硅烷反应，在6-APA6位的氨基上形成三甲硅基，然后和N-甲酰基氮杂革在三乙胺存在下反应，得到美西林。

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美西林文献

Fluorescence anisotropy-based measurement of Pseudomonas aeruginosa penicillin-binding protein 2 transpeptidase inhibitor acylation rate constants.

Anal. Biochem. 463 , 15-22, (2014)

High-molecular-weight penicillin-binding proteins (PBPs) are essential integral membrane proteins of the bacterial cytoplasmic membrane responsible for biosynthesis of peptidoglycan. They are the targ...

The Rcs phosphorelay is a cell envelope stress response activated by peptidoglycan stress and contributes to intrinsic antibiotic resistance.

J. Bacteriol. 190(6) , 2065-74, (2008)

Gram-negative bacteria possess stress responses to maintain the integrity of the cell envelope. Stress sensors monitor outer membrane permeability, envelope protein folding, and energization of the in...

The bacterial actin MreB rotates, and rotation depends on cell-wall assembly.

Proc. Natl. Acad. Sci. U. S. A. 108(38) , 15822-7, (2011)

Bacterial cells possess multiple cytoskeletal proteins involved in a wide range of cellular processes. These cytoskeletal proteins are dynamic, but the driving forces and cellular functions of these d...

更多文献

美西林

美西林用途

美西林名称

美西林生物活性

美西林物理化学性质

美西林毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

美西林安全信息

美西林合成路线

详细合成路线

美西林上下游产品

美西林上游产品

美西林下游产品

美西林制备

美西林文献

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