Amifloxacin

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Chemical Structure| 86393-37-5 同义名 : Win49375
CAS号 : 86393-37-5
货号 : A749227
分子式 : C16H19FN4O3
纯度 : 97%
分子量 : 334.346
MDL号 : MFCD00864981
存储条件:

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 50 mg/mL(149.55 mM),配合低频超声,并调节pH至11

动物实验配方:
生物活性
描述 Amifloxacin (Win49375), a synthetic antibacterial agent of the quinolone class, is highly active by the oral route, with 50% effective doses within two- to threefold of those obtained with parenteral medication. When mice infected intraperitoneally with E. coli Vogel are medicated at 0.5-h postinfection subcutaneously, intravenously, or orally the ED50s for Amifloxacin are 0.6, 0.8, and 1.0 mg/kg, respectively[1]. Amifloxacin inhibited Branhamella, Haemophilus, and Neisseria at less than or equal to 0.25 mg/ml, and 90% of Pseudomonas aeruginosa, including gentamicin- and carbenicillin-resistant isolates, at 4 mg/ml. It also inhibited staphylococci, including methicillin-resistant isolates, but was less active against streptococci and Bacteroides species. Amifloxacin had in vitro activity similar to enoxacin, ofloxacin, and norfloxacin, but was less active than ciprofloxacin[2]. Amifloxacin showed potent inhibitory activity against DNA gyrase of Escherichia coli. Cell lysis was induced with combined treatment of amifloxacin and sodium dodecyl sulfate in E. coli. The frequency of mutants spontaneously resistant to amifloxacin was extremely low in all species tested[3]. For amikacin-resistant P aeruginosa, the minimal inhibitory concentrations (MICs) of amifloxacin ranged from 1 to 16 mg/ml. For all strains tested, microbial susceptibilities to amifloxacin were greater than those to currently available oral antimicrobial drugs, such as cinoxacin and trimethoprim[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.95mL

2.99mL

1.50mL

29.91mL

5.98mL

2.99mL

参考文献

[1]Cornett JB, Wagner RB, Dobson RA, Wentland MP, Bailey DM. In vitro and in vivo antibacterial activities of the fluoroquinolone WIN 49375 (amifloxacin). Antimicrob Agents Chemother. 1985 Jan;27(1):4-10

[2]Neu HC, Labthavikul P. Antibacterial activity of amifloxacin (WIN 49, 375), a new quinolone agent. Diagn Microbiol Infect Dis. 1985 Nov;3(6):469-78

[3]Watanabe M, Inoue M, Mitsuhashi S. In vitro activity of amifloxacin against outer membrane mutants of the family Enterobacteriaceae and frequency of spontaneous resistance. Antimicrob Agents Chemother. 1989 Nov;33(11):1837-40

[4]Baltch AL, Sutphen NT, Smith RP, Conley PE. Inhibitory and bactericidal activities of amifloxacin, a new quinolone carboxylic acid, compared with those of seven other antimicrobial agents. Clin Ther. 1984;7(1):73-80