罗红霉素

罗红霉素用途

Roxithromycin是半合成的大环内酯类抗生素。

罗红霉素作用

罗红霉素是一种半合成的14元环大环内酯类抗生素。其作用机理与红霉素相似，体内抗菌作用比红霉素强1-4倍，对革兰阳性菌的作用较红霉素略差，对嗜肺军团菌的作用较红霉素强，对肺炎衣原体、肺炎支原体、溶脲脲原体的抗微生物作用与红霉素相仿或略强。
本品可透过细菌细胞膜，在接近供体(“P”位)与细菌核糖体的50S亚基成可逆性结合，阻断了转移核糖核酸结合至“P”位上，同时也阻断了多肽链自受位(“A”位)至“P”位的转移，因而细菌蛋白质合成受到抑制，从而起抗菌作用。其特点是能较快进入巨噬细胞、肺泡细胞、中性粒细胞内。体外研究证实，罗红霉素的抗菌谱广，对各种链球菌（包括A、B、C型链球菌和肺炎链球菌，但G型和肠球菌除外）、肺炎链球菌、金葡菌、金黄色葡萄球菌(MRSA除外)、表皮葡萄球菌、嗜肺军团菌、杜克雷嗜血杆菌、沙眼衣原体、肺炎支原体、口腔或阴道厌氧菌的抗菌活性与红霉素几乎相同，卡他布兰汉球菌对罗红霉素高度敏感，对弯曲杆菌、百日咳杆菌、流感嗜血杆菌、结核杆菌、白喉杆菌，也有抑制作用，对其他革兰阴性菌无抗菌活性。本品的体内抗菌活性明显强于红霉素，且对衣原体、支原体、溶脲脲原体、梅毒螺旋体及军团菌感染疗效显著。对螺旋杆菌、淋球菌、脑膜炎球菌、百日咳杆菌等作用较弱。某些细菌对红霉素与本品有交叉耐药性。

罗红霉素名称

[ CAS 号 ]:
80214-83-1

[ 中文名 ]:
罗红霉素

[ 英文名 ]:
Roxithromycin

[中文别名 ]:

9-[O-(2-甲氧基乙氧基)甲肟]红霉素

[英文别名 ]:

Roxid
Overal
Forilin
MFCD00214389
Roxithromycin
Claramid
biaxsig
RU 965
Assoral
roxyithromycin

罗红霉素生物活性

[ 描述 ]:

Roxithromycin是半合成的大环内酯类抗生素。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[参考文献]

[1]. http://en.wikipedia.org/wiki/Roxithromycin

[相关活性小分子]

罗红霉素物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
864.7±75.0 °C at 760 mmHg

[ 熔点 ]:
115- 120ºC

[ 分子式 ]:
C₄₁H₇₆N₂O₁₅

[ 分子量 ]:
837.047

[ 闪点 ]:
476.7±37.1 °C

[ 精确质量 ]:
836.524597

[ PSA ]:
216.89000

[ LogP ]:
3.73

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.535

[ 储存条件 ]:
2-8°C

罗红霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KF4990000

CHEMICAL NAME :: Erythromycin, 9-O-((2-methoxyethoxy)methyl)oxime

CAS REGISTRY NUMBER :: 80214-83-1

LAST UPDATED :: 199806

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C41-H76-N2-O15

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 :: 830 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes 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: 36(Suppl 4),94,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 665 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1471,1995

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: .2 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1471,1995

罗红霉素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
26

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

[ RTECS号 ]:
KF4990000

[ 海关编码 ]:
2941500000

罗红霉素合成路线

详细合成路线

罗红霉素上下游产品

罗红霉素上游产品

罗红霉素下游产品

罗红霉素制备

以红霉素为原料，和盐酸羟胺在三乙胺和甲醇中反应，生成肟，然后和甲氧基乙氧基甲基氯在丙酮中反应，即得罗红霉素。

罗红霉素海关

[ 海关编码 ]: 2941500000

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