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头孢布烯

头孢布烯用途

Ceftibuten(Sch39720)是第三代头孢菌素类抗生素。

头孢布烯名称

[ CAS 号 ]:
97519-39-6

[ 中文名 ]:
头孢布坦

[ 英文名 ]:
Ceftibuten

[中文别名 ]:

[英文别名 ]:

7432 S
s7432
cis-Ceftibutin
ceftibutenum [INN_la]
Ceftibutene
antibiotic7432s
7432S
Seftem
Antibiotic 7432S
cephem

头孢布烯生物活性

[ 描述 ]:

Ceftibuten(Sch39720)是第三代头孢菌素类抗生素。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

天然产物 >> 生物碱

[参考文献]

[1]. Wise R, et al. Ceftibuten--in-vitro activity against respiratory pathogens, beta-lactamase stability and mechanism of action. J Antimicrob Chemother, 1990. 26(2): p. 209-213.

[相关活性小分子]

头孢布烯物理化学性质

[ 密度 ]:
1.8±0.1 g/cm3

[ 沸点 ]:
966.4±65.0 °C at 760 mmHg

[ 分子式 ]:
C₁₅H₁₄N₄O₆S₂

[ 分子量 ]:
410.425

[ 闪点 ]:
538.3±34.3 °C

[ 精确质量 ]:
410.035461

[ PSA ]:
216.46000

[ LogP ]:
-0.96

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.762

[ 储存条件 ]:
2-8℃

头孢布烯MSDS

详细MSDS(安全技术说明书)

头孢布烯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XI0367220

CHEMICAL NAME :: 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((2-(2-amino-4-thiazolyl)- 4-carboxy-1-oxo-2-butenyl)amino)-8-oxo-, (6R-(6-alpha,7-beta(Z)))-

CAS REGISTRY NUMBER :: 97519-39-6

LAST UPDATED :: 199509

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C15-H14-N4-O6-S2

MOLECULAR WEIGHT :: 410.45

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 - muscle weakness Gastrointestinal - hypermotility, diarrhea Gastrointestinal - other changes

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),804,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),804,1989 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35 gm/kg/35D-I

TOXIC EFFECTS :: Gastrointestinal - other changes Kidney, Ureter, Bladder - urine volume decreased Biochemical - Metabolism (Intermediary) - other proteins

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),816,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 273 gm/kg/13W-I

TOXIC EFFECTS :: Gastrointestinal - other changes Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),858,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 54600 mg/kg/26W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume decreased Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in erythrocyte (RBC) count

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),919,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 72800 mg/kg/13W-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),883,1989 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 12500 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 39,253,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 11 gm/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),990,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 12500 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),1040,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 520 mg/kg

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

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 37(Suppl 1),1026,1989

头孢布烯制备

化合物(I)和甲酸二苯甲基酯溶于四氢呋喃，在氢化钠存在下，于0～20℃下反应2h，可得高收率的化合物(1I)。(Ⅱ)再和有机磷试剂进行Wittig反应，生成化合物(Ⅲ)，其E/Z=3/2。接着用三氟乙酸在二氯甲烷中，于0～5℃下反应1.5h，水解得到化合物(Ⅳ)。然后和头孢菌素(V)，按常法，即在三氯氧磷和N一甲基吗啉存在下，在二氯甲烷中，于-20℃下反应20min，得到化合物(Ⅵ)，其E/Z=85/15。最后在三氯化铝存在下，在苯甲醚中加热，可得头孢布烯及其E式异构体，其E／Z=85／15。但该顺反异构体混合物在Ph值为3--4的水溶液中，因E式会异构化为Z式，缓慢结晶出Z式的同时，E式不断地异构化，因而可得到高收率的头孢布烯。