Clinafloxacin  (Synonyms: 克林沙星; AM-1091; CI-960; PD 127391)

Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro^[1]. Clinafloxacin is against DNA gyrase and topoisomerase IV of?S. aureus with IC₅₀ values of 0.92 μg/ml and 1.62 μg/ml, respectively^[2].

Clinafloxacin exhibits activity against S. pneumonia with an MIC of 1μg/ml for the parC-gyrA mutants^[2].
Clinafloxacin hydrochloride has antibacterial activities against target-altered mutant strains of?S. aureus. It against Wild type S. aureus, gyrA?mutant S. aureus and gyrA?mutant S. aureus with MIC values of 0.016 μg/ml, 0.063 μg/ml and 0.915 μg/ml, respectively^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

365.79

C₁₇H₁₇ClFN₃O₃

105956-97-6

固体

Light yellow to brown

克林沙星

Room temperature in continental US; may vary elsewhere.

• [1]. M Takei, et al. Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition.Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.  [Content Brief]

  [2]. Randa H Abdelkreem, et al. DNA Gyrase and Topoisomerase IV Mutations and their effect on Quinolones Resistant Proteus mirabilis among UTIs Patients. Pak J Med Sci. Sep-Oct 2020;36(6):1234-1240.  [Content Brief]

  [3]. A Domenech, et al. Experimental study of clinafloxacin alone and in combination in the treatment of ciprofloxacin-susceptible and -resistant pneumococcal meningitis.Microb Drug Resist. 2003;9 Suppl 1:S53-9.  [Content Brief]