盐酸头孢唑兰

中文名称:

盐酸头孢唑兰

中文同义词:

盐酸头孢唑兰;头孢唑兰盐酸盐;1-[[(6R,7R)-7-[(Z)-2-(5-氨基-1,2,4-噻二唑-3-基)-2-甲氧亚氨基乙酰胺基]-2-羧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-3-基]甲基]咪唑并[1,2-b]哒嗪鎓内盐盐酸盐;1-[[(6R,7R)-7-[(Z)-2-(5-氨基-1,2,4-噻二唑-3-基)-2-甲氧亚氨基乙酰胺基]-2-羧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-3-基]甲基]咪唑并[1,2-B]哒嗪内盐盐酸盐

英文名称:

Cefozopran hydrochloride

英文同义词:

Cefozopran hydrochloride;(6R,7R)-7-[[(2E)-2-(5-Amino-1,2,4-thiadiazol-3-yl)-2-methoxyiminoacetyl]amino]-3-(imidazo[2,3-f]pyridazin-4-ium-1-ylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid chloride;Cefozopran hydrochloride (jp15);Czop;D02233;Firstcin (tn);Cefozopran hydrochlo;SCE-2787 hydrochloride

CAS号:

113981-44-5

分子式:

C19H17N9O5S2.HCl

分子量:

551.99

EINECS号:

1806241-263-5

相关类别:

盐酸头孢唑兰及其中间体;药物杂质及中间体;医药原料药;医药、农药及染料中间体;Cefozopran Hydrochloride and its intermediates

Mol文件:

Mol File

储存条件 

Inert atmosphere,2-8°C

概述

盐酸头孢唑兰(cefozopran hydrochloride)是日本武田药品工业公司研发的第四代注射用头孢菌素，目前在日本已作为院外感染初期的首选药物被广泛应用于包括新生儿感染在内的各科感染症的治疗。除了MRSA外，它具有广谱活性，对革兰阳性菌的活性总体上优于头孢他啶、头孢毗肟和氟氧头孢，而与头孢匹罗相当，对革兰阴性菌与上述对照药具有同等的活性。它对β?内酰胺酶有高度的稳定性，体内分布广泛，血浆和组织浓度较高，大部分以原药形式从尿中排泄．24h尿排泄率80%～90%，无体内蓄积倾向。盐酸头孢唑兰的化学名称为：[[(6R,7R)-7-[(Z)-2-(5-氨基-1,2,4-噻二唑-3-基)-2-甲氧亚氨基乙酰氨基]-2-羧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-3-基]甲基]咪唑并[1,2-b]哒嗪鎓氢氧化物内盐单盐酸盐。

生物活性

Cefozopran (SCE-2787) hydrochloride 是一种半合成的、非肠道的、第四代头孢菌素。Cefozopran hydrochloride，作为一种抗生素，具有广谱抗菌活性，能抑制大多数革兰氏阴性和革兰氏阳性菌。

体外研究

Cefozopran (SCE-2787) is a fourth-generation cephalosporin that has good activity against gram-positive organisms including methicillin-susceptible staphylococci, enterococci, and viridans group streptococci; and against gram-negative organisms including hemophilus influenza. Moreover, cefozopran has comparatively good activity against enterococci and P. aeruginosa , which are refractory to other cephalosporins.

体内研究

Cefozopran (SCE-2787) (5-80 mg/kg; s.c.; twice a day for 5 days; four-week-old ICR male mice) is effective against acute respiratory tract infections caused by Kiebsiella pneumonia DT-S. In the model of chronic respiratory tract infection caused by K. pneumoniae 27, Cefozopran (20-80 mg/kg; s.c.; twice a day for 7 days; five-week-old CBA/J female mice) is as effective as Ceftazidime.

用途 

抗感染

用途 

盐酸头孢唑兰适用于葡萄球菌、链球菌、肠球菌、消化链球菌、大肠杆菌、肠杆菌、沙雷氏菌、克雷白氏菌、枸橼酸杆菌、变形杆菌、假单孢菌、流感杆菌、不动杆菌、拟杆菌中对盐酸头孢唑兰敏感菌引起的败血症，外伤感染，呼吸系统、泌尿系统及腹腔、盆腔内化脓性炎症，眼科和耳鼻喉科炎症等。