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105956-99-8

中文名稱 鹽酸克林沙星
英文名稱 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 2024/11/06 17:53:20
105956-99-8 結(jié)構(gòu)式 105956-99-8 結(jié)構(gòu)式

基本信息

中文別名
鹽酸克林沙星
克林沙星鹽酸鹽
包被鹽酸可林沙星
7-(3-氨基-1-吡咯烷基)-8-氯-1-環(huán)丙基-6-氟-1,4-二氫-4-氧代-3-喹啉羧酸鹽酸鹽
英文別名
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
所屬類別
原料藥:喹諾酮類藥

物理化學(xué)性質(zhì)

熔點(diǎn)162-168°C
儲(chǔ)存條件Refrigerator
溶解度DMSO(微溶)、甲醇(微溶)、水(微溶、加熱)
形態(tài)固體
顏色淡黃色至淡黃色
穩(wěn)定性吸濕性

常見問題列表

生物活性
Clinafloxacin hydrochloride (AM 1091 hydrochloride) 是一種高效廣譜氟喹諾酮類抗生素 (antibiotic),對(duì)革蘭氏陽性、革蘭氏陰性和厭氧病原體均有抑制活性。Clinafloxacin hydrochloride 對(duì)金黃色葡萄球菌的DNA促旋酶 (DNA gyrase) 和拓?fù)洚悩?gòu)酶 IV (topoisomerase IV) 有抑制作用,IC50 值分別為 0.92 μg/ml 和 1.62 μg/ml。
靶點(diǎn)

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

體外研究

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.

體內(nèi)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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