中文同义词:
双氯西林钠;双氟西林;双氯青霉素钠一水合物;(2S,5R,6R)-3,3-二甲基-6-[5-甲基-3-(2,6-二氯苯基)-4-异唑甲酰氨基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-甲酸钠;(2S,5R,6R)-3,3-二甲基-6-[5-甲基-3-(2,6-二氯苯基)-4-异噁唑甲酰氨基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-甲酸钠;双氯苯唑青霉素钠;双氯青霉素钠;双氯西林钠水合物
英文名称:
Dicloxacillin sodium
英文同义词:
3-(2,6-DICHLOROPHENYL)-5-METHYL-4-ISOXAZOLYL PENICILLIN;DICLOXACILLIN SODIUM SALT HYDRATE VETRAN;DICLOXACILLIN SODIUM EPD(CRM STANDARD);DICLOXACILLIN SODIUM USP(CRM STANDARD);DICLOXACILLIN SODIUM WHO(CRM STANDARD);Dicloxacillin monohydrate sodium salt;Dicloxacillin sodium;Sodium 7-[3-(2,6-dichlorophenyl)-5-methyl-oxazol-4-yl]carbonylamino-3,3-dimet hyl-6-oxo-2-thia-5-azabicyclo[3.2.0]heptane-4-carboxylate
相关类别:
青霉素类;医药原料药;小分子抑制剂;抗生素;原料;Diclocil;APIs;A - KAntibiotics;Antibacterial;Antibiotics A to;Antibiotics A-FAntibiotics;Peptide Synthesis/Antibiotics;Aromatics;Chiral Reagents;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;Sulfur Selenium Compounds;Chemical Structure Class;Interferes with Cell Wall SynthesisAntibiotics;Mechanism of Action;Penicillins and Cephalosporins (beta-Lactams);Spectrum of Activity
CAS 数据库
13412-64-1(CAS DataBase Reference)
用途
阿莫西林/双氯西林钠分散片为阿莫西林(Amoxillin)与双氯西林(Dicloxacillin)钠的复方制剂。阿莫西林系广谱半合成青霉素,对各种革兰阳性菌、阴性菌均有较强的抗菌活性;双氯西林为耐酶的青霉素类抗生素,能抑制细菌产生的β-内酰胺酶活性,增强阿莫西林的抗菌作用。
生物活性
Dicloxacillin Sodium hydrate (Dicloxacillin sodium salt monohydrate) 是青霉素类的窄谱β内酰胺抗生素, 可用于革兰氏阳性菌感染的研究, 有效对抗β-内酰胺酶产生的微生物如金黄色葡萄球菌。
体外研究
Dicloxacillin exhibits EC 50 values of 0.06 and 0.50 mg/L in ATCC 25923 and E19977, respectively. Dicloxacillin exhibits MIC values of 0.125 and 0.5 mg/L in ATCC 25923 and E19977 with pH 7.4, respectively.
Cell Viability Assay
Cell Line: Strains ATCC 25923 and E19977.
Concentration: 0-500 mg/L.
Incubation Time: Up to 24 h.
Result: Exhibited EC 50 values of 0.06 and 0.50 mg/L in ATCC 25923 and E19977, respectively.
Cell Line:
Strains ATCC 25923 and E19977.
Concentration:
0-500 mg/L.
Incubation Time:
Up to 24 h.
Result:
Exhibited EC 50 values of 0.06 and 0.50 mg/L in ATCC 25923 and E19977, respectively.
体内研究
Dicloxacillin exhibits therapeutic activity in murine peritonitis-sepsis model and all the mice are survivied.
Animal Model: Female outbred Swiss Webster mice (Murine peritonitis-sepsis model).
Dosage: 125 mg/kg.
Administration: IV injection, single doses.
Result: All the mice survived.
Animal Model:
Female outbred Swiss Webster mice (Murine peritonitis-sepsis model).
Administration:
IV injection, single doses.
Result:
All the mice survived.
化学性质
白色或淡黄色结晶性粉末。熔点222-225℃(分解)。易溶于水,溶于甲醇、乙醇,对酸稳定。有异臭,味苦。
用途
抗菌素类药,用于对青霉素G耐药的金葡菌的感染。
生产方法
由邻硝基甲苯经氯化、还原、重氮化、置换、氯化、肟化、氯化、环合、水解、氯化,得到3-(2,6-二氯苯基)-5-甲基-4-异噁唑酰氯,再与6-APA缩合得到双氯西林([3116-76-5]),最后用异辛酸钠成盐得到双氯西林钠。
毒性
LD50 in mice (g/kg): 0.9 i.v.; in rats (g/kg): 0.63 i.p.; >5 orally (Gloxhuber)