Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinoloneantibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro^[1]. Clinafloxacin is againstDNA gyraseandtopoisomeraseIVof S. aureuswithIC₅₀values of 0.92 μg/ml and 1.62 μg/ml, respectively^[2].

Clinafloxacin exhibits activity againstS. pneumoniawith anMICof 1μg/ml for the parC-gyrA mutants^[2].
Clinafloxacin hydrochloride has antibacterial activities against target-altered mutant strains of S. aureus. It against Wild typeS. aureus,gyrA mutantS. aureusandgyrA mutantS. aureuswith MIC values of 0.016 μg/ml, 0.063 μg/ml and 0.915 μg/ml, respectively^[3].

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].

365.79

Solid

C₁₇H₁₇ClFN₃O₃

105956-97-6

克林沙星

Room temperature in continental US; may vary elsewhere.

DMSO : 2 mg/mL(5.47 mM;ultrasonic and warming and heat to 80℃)

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