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拉氧头孢

拉氧头孢用途

莫沙内酰胺(Latamoxef)是一种合成的氧-β-内酰胺抗生素。内酰胺对革兰氏阳性和革兰氏阴性需氧和厌氧细菌具有广泛的活性。莫沙内酰胺抑制β-内酰胺酶的产生[1]。

拉氧头孢名称

[ CAS 号 ]:
64952-97-2

[ 中文名 ]:
拉氧头孢

[ 英文名 ]:
Latamoxef

[中文别名 ]:

头霉拉坦

[英文别名 ]:

Latamoxef
lamoxactam
(R)-Moxalactam
Listeria MOX Supplement,Moxalactam
Oxa-cephem
LMOX

拉氧头孢生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

β-lactamases[1]

[体外研究]

莫沙内酰胺(Latamoxef)抑制90%的大肠杆菌、克雷伯菌属、变形杆菌属、Morganella morganii、淋病奈瑟菌、脑膜炎奈瑟菌、流感嗜血杆菌和沙门氏菌属菌株,包括浓度低于1μg/mL时对头孢噻吩(HY-B1275A)和庆大霉素(HY-A0276A)耐药的菌株[1]。莫沙内酰胺对铜绿假单胞菌具有中等活性,通常对其他假单胞杆菌具有活性,不动杆菌通常对莫沙内酮具有耐药性[1]。莫沙内酰胺在体外对多种β-内酰胺酶(包括脆弱芽孢杆菌产生的酶)具有显著的稳定性,可抑制β-内糖酶的产生,且不会诱导I类β-内酯酶[1]。

[体内研究]

莫沙内酰胺(Latamoxef)(0-7.4 mg/小鼠；皮下注射；一次)对小鼠细菌感染有效[2]。动物模型：4周龄雄性ICR小鼠,体重18-20g,细菌感染模型[2]剂量：0-7.4mg/小鼠给药：皮下注射,一次。结果：ED50s小于7.4mg/鼠对革兰氏阳性和革兰氏阴性细菌感染小鼠具有保护作用。

[参考文献]

[1]. Carmine AA, et al. Moxalactam (latamoxef). A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1983 Oct;26(4):279-333.

[2]. Goto S. In vitro and in vivo antibacterial activity of moxalactam, an oxa-β-lactam antibiotic. Clinical Infectious Diseases, 1982, 4(Supplement_3): S501-S510.

拉氧头孢物理化学性质

[ 密度 ]:
1.77 g/cm3

[ 沸点 ]:
836ºC

[ 熔点 ]:
117 - 122ºC

[ 分子式 ]:
C₂₀H₂₀N₆O₉S

[ 分子量 ]:
520.47300

[ 精确质量 ]:
520.10100

[ PSA ]:
231.60000

[ 折射率 ]:
1.768

[ 储存条件 ]:
-20°C，密闭，干燥

拉氧头孢毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RN6824500

CHEMICAL NAME :: 5-Oxa-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((carboxy(4-hydroxyphenyl)acetyl) amino)-7-methoxy-3-(((1-methyl-1H-tetrazol-5-yl)thio) methyl)-8-oxo-

CAS REGISTRY NUMBER :: 64952-97-2

LAST UPDATED :: 199504

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C20-H20-N6-O9-S

MOLECULAR WEIGHT :: 520.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 480 mg/kg/4D-I

TOXIC EFFECTS :: Blood - hemorrhage

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 99,126,1983 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5300 No. of Facilities: 69 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 5145 (estimated) No. of Female Employees: 4707 (estimated)

拉氧头孢安全信息

[ 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

[ WGK德国 ]:
3

[ RTECS号 ]:
RN6824500

拉氧头孢文献

A potential substrate binding conformation of β-lactams and insight into the broad spectrum of NDM-1 activity.

Antimicrob. Agents Chemother. 56(10) , 5157-63, (2012)

New Delhi metallo-β-lactamase 1 (NDM-1) is a key enzyme that the pathogen Klebsiella pneumonia uses to hydrolyze almost all β-lactam antibiotics. It is currently unclear why NDM-1 has a broad spectrum...

Comparison of cefoxitin and moxalactam 30 microg disc diffusion methods for detection of methicillin resistance in coagulase-negative staphylococci.

J. Antimicrob. Chemother. 59(4) , 763-6, (2007)

To compare cefoxitin and/or moxalactam 30 microg disc diffusion (DD) methods to detect methicillin resistance in coagulase-negative staphylococci (CoNS) using both high- and low-density (HD/LD) inocul...

Phosphate deprivation is associated with high resistance to latamoxef of gel-entrapped, sessile-like Escherichia coli cells.

J. Antimicrob. Chemother. 49(2) , 315-20, (2002)

Viable Escherichia coli cells were entrapped in agar gel layers and incubated in a phosphate-limited glucose medium. Immobilized bacteria displayed enhanced alkaline phosphatase activity and overexpre...

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