盐酸头孢卡品酯
中文名称:
盐酸头孢卡品酯
中文同义词:
7-[2-(2-氨基-1,3-噻唑-4-基)戊-3-烯酰胺基]-3-(氨基甲酰氧甲基)-8-氧代-5-硫-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸 2,2-二甲基丙酰氧甲基酯盐酸盐;盐酸头孢卡品酯;盐酸头孢卡品酯水合物;头孢卡品酯系列/硫酸头孢卡品酯;盐酸头孢卡品酯 一水合物;头孢卡品酯系列
英文名称:
Cefcapene pivoxil hydrochloride
英文同义词:
2,2-dimethylpropanoyloxymethyl 7-[2-(2-amino-1,3-thiazol-4-yl)pent-2-enoylamino]-3-(carbamoyloxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate;CEFCAPENE PIVOXIL HCL;Cefcapene pivoxil hydrochloride;5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 3-(((aminocarbonyl)oxy)methyl)-7-((2-(2-amino-4-thiazolyl)-1-oxo-2-pentenyl)amino)-8-oxo-, (2,2-dimethyl-1-oxopropoxy)methyl ester,(6R-(6-alpha,7-beta(Z)))-, monohydrochloride, hydrate;Cefcapene Pivoxil Hydrochloride Monohydrate;(6R,7R)-3-[[(Aminocarbonyl)oxy]methyl]-7-[[(2Z)-2-(2-amino-4-thiazolyl)-1-oxo-2-pentenyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic Acid, (2,2-Dimethyl-1-oxopropoxy)methyl Ester Hydrochloride;Flomox;Cefcapene pivoxil hydrochloride hydrate
CAS号:
147816-24-8
分子式:
C23H32ClN5O9S2
分子量:
622.11
EINECS号:
1592732-453-0
相关类别:
原料药;中间体;合成;药物杂质及中间体;医药原料;原料;化工原料;化学试剂;Intermediates Fine Chemicals;Chiral Reagents;Pharmaceuticals;Sulfur Selenium Compounds
Mol文件:
147816-24-8.mol
熔点
158-164°C
储存条件
Keep in dark place,Inert atmosphere,2-8°C
InChIKey
LUXIJPQYUCFVAL-XRLCNELCSA-N
CAS 数据库
147816-24-8
药理作用及作用机制
盐酸头孢卡品酯是第四代可口服头孢类抗生素，药理研究表明，对好氧革兰阳性菌的MSSA的MIC80为3.13μg/mL，与头孢替安、头孢克洛相同、对肺炎链球菌的MIC80≤0.1μg/mL，优于头孢克洛，与头孢托仑相当，对耐青霉素的肺炎链球菌的活性很强，MIC80为0.78μg/mL。对革兰阴性菌中的弗氏柠檬酸杆菌、阴沟肠杆菌、雷氏普罗威登斯菌、黏膜炎布兰汉氏球菌、黏质沙雷菌比头孢托仑、头孢替安强。对变形杆菌属、流感嗜血杆菌、摩氏摩根氏菌、淋球菌的活性比头孢克洛、头孢替安强，与头孢特仑相当。对耐氨苄西林的流感嗜血杆菌有很强的活性，MIC80为0.05μg/mL。
药代动力学
口服后在肠道中经酯酶水解，生成活性的头孢菌素化合物S-1006，新戊酸和甲醛。
适应症
盐酸头孢卡品酯第三代具有抗厌氧菌活性的口服头孢菌素，适用于对本品敏感的链球菌属、葡萄球菌属、淋球菌属等引起的感染
生物活性
Cefcapene pivoxil hydrochloride hydrate 是第 3 代头孢菌素的前药形式，具有口服活性和广谱抗菌 (anti-bacterial) 活性。Cefcapene pivoxil hydrochlorid hydrate 用于掌跖脓疱病 (PPP) 等感染性疾病的研究。
靶点
IC50: bacterial
体内研究
Cefcapene pivoxil hydrochloride hydrate (oral administration; 100mg/kg; 4 days) is effective against invasive BLNAR strains in mice lung, it stimates peak antibiotic concentrations of 1 to 2 μg/ml in the blood of mice from 30 to 120 min after intragastric administration.
Animal Model: Four-week-old female C57BL/6J mice with bacterial suspension in BSG (1×10 9 CFU)
Dosage: 100 mg/kg
Administration: Oral administration; 100mg/kg; 4 days
Result: Was against H. influenzae colonization in mouse lung.
Animal Model:
Four-week-old female C57BL/6J mice with bacterial suspension in BSG (1×10 9 CFU)
Dosage:
100 mg/kg
Administration:
Oral administration; 100mg/kg; 4 days
Result:
Was against H. influenzae colonization in mouse lung.
RTECS号
XI0325000
