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105956-99-8

中文名称 盐酸克林沙星
英文名称 Clinafloxacin hydrochloride
CAS 105956-99-8
分子式 C17H18Cl2FN3O3
分子量 402.25
MOL 文件 105956-99-8.mol
更新日期 2024/07/11 10:51:59
105956-99-8 结构式 105956-99-8 结构式

基本信息

中文别名
盐酸克林沙星
克林沙星盐酸盐
包被盐酸可林沙星
7-(3-氨基-1-吡咯烷基)-8-氯-1-环丙基-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸盐酸盐
英文别名
M 1091
KR 11095
ClinafoxacinHCl
CLINAFLOXACIN HCL
Clinafloxacinhydrochloride
CLINANFLOXACIN HYDROCHLORIDE
HYDROGEN CLINAFLOXACIN CHLORIDE
Clinafloxacin hydrochloride USP/EP/BP
7-(3-aminopyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid hydrochloride
7-(3-azanylpyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-quinoline-3-carboxylic acid hydrochloride
所属类别
原料药:喹诺酮类药

物理化学性质

熔点162-168°C
储存条件Refrigerator
溶解度DMSO(微溶)、甲醇(微溶)、水(微溶、加热)
形态固体
颜色淡黄色至淡黄色
稳定性吸湿性

常见问题列表

生物活性
Clinafloxacin hydrochloride (AM 1091 hydrochloride) 是一种高效广谱氟喹诺酮类抗生素 (antibiotic),对革兰氏阳性、革兰氏阴性和厌氧病原体均有抑制活性。Clinafloxacin hydrochloride 对金黄色葡萄球菌的DNA促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 有抑制作用,IC50 值分别为 0.92 µg/ml 和 1.62 µg/ml。
靶点

MIC: 1 μg/ml (parC-gyrA mutants, S. pneumonia )

体外研究

Clinafloxacin exhibits activity against S. pneumonia with an MIC of 1μg/ml for the parC-gyrA mutants.Clinafloxacin hydrochloride has antibacterial activities against target-altered mutant strains of S. aureus . It against Wild type S. aureus , gyr A mutant S. aureus and gyr A mutant S. aureus with MIC values of 0.016 µg/ml, 0.063 µg/ml and 0.915 µg/ml, respectively.

体内研究

Clinafloxacin is very effective for the therapy of penicillin-resistant, ciprofloxacin-susceptible pneumococcal meningitis in the rabbit model. With the CS strain (2349)(Clinafloxacin MIC=0.12 μg/ml), at a dose of 10 mg/kg and 20 mg/kg per day Clinafloxacin achieves an initial reduction at 6 hr. Both are bactericidal at this point but presents regrowth at 24 hr, and the final reduction at 24 hr in mean log cfu/ml is 22.30 and 23.83, respectively. However, With the CR strain (4371)(Clinafloxacin MIC=0.5 μg/ml), Clinafloxacin even at 20 mg/kg per day does not decrease bacterial titers at any time point in this rabbit model of meningitis.

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