Amifloxacin

Research use only, not for human use.

Amifloxacin is a synthetic antibacterial compound and showed moderate activity against Staphylococcus aureus, with MICs of less than or equal to 2 micrograms/ml.

Amifloxacin is a synthetic antibacterial compound and showed moderate activity against Staphylococcus aureus, with MICs of less than or equal to 2 micrograms/ml.(In Vitro):The activity of Amifloxacin in vitro was comparable to those of norfloxacin and pefloxacin against Enterobacteriaceae and generally greater than those of tobramycin and cefotaxime. Amifloxacin was more active in vitro than carbenicillin and mezlocillin against Pseudomonas aeruginosa isolates.(In Vivo):Against systemic, gram-negative bacterial infections in mice, Amifloxacin was generally less active than cefotaxime but more active than gentamicin. WIN 49548, the major piperazinyl-N-desmethyl metabolite of Amifloxacin, was aa effective as the parent drug against experimental infections in mice when given parenterally. When administered orally, however, this metabolite was less potent than Amifloxacin. Amifloxacin was highly active by the oral route, with 50% effective doses within two- to threefold of those obtained with parenteral medication.

Amifloxacin (WIN 49375) is active in vitro against Pseudomonas aeruginosa isolates and shows moderate activity against Staphylococcus aureus, with MICs of less than or equal to 2 μg/mL.

Amifloxacin (WIN 49375) is highly active by the oral route, with 50% effective doses within two- to threefold of those obtained with parenteral medication. The effectiveness of Amifloxacin with various routes of medication is demonstrated with these experimental infections. 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. Blood radioactivity peaks at 0.5 h after oral administration of [14C]Amifloxacin mesylate to rats at 20 mg/kg and is equivalent to 7.1±0.26 μg of Amifloxacin per mL. From 0.75 to 4 h, blood radioactivity decreases rapidly from 7.0±0.25 μg/mL to 1.2±0.12 μg/mL. Between 8 and 48 h the rate of decline in blood radioactivity slows and is more complex. At 48 h, the blood radioactivity is equivalent to 0.14±0.02 μg/mL. Blood levels of radioactivity after i.v. administration of [14C]Amifloxacin mesylate to rats at 20 mg/kg decrease from 29.1±0.85 μg/mL at 1.0 min to 14.4±0.52 μg/mL at 10 min. From 0.25 to 4 h blood radioactivity decreases from 13.0±0.42 μg/mL to 0.97±0.09 μg/mL in a log-linear manner. The rate of elimination from 4 to 24 h is slower and more complex. At 24 h, blood radioactivity is equivalent to 0.12±0.01 ug/mL.

Win49375

GPCR/G Protein

Antibacterial

Nucleoside Antimetabolite/Analog

——

——

86393-37-5

334.351

C16H19FN4O3

>98% (HPLC)

In Vitro:?H2O : 50 mg/mL (149.54 mM)

CNn1cc(C(O)=O)c(=O)c2cc(F)c(cc12)N1CCN(C)CC1

——

(-20℃)

With Ice Pack

≥ 2 years