In Vitro Antibacterial Activity of a New Quinolone, NM394

Ozaki, Masakuni; Matsuda, Masato; Tomii, Yoshifumi; Kimura, Kiyoshi; Kazuno, Kenji; Kitano, Masahiko; Kise, Masahiro; Shibata, Kazuo; Otsuki, Masako; Nishino, Takeshi

doi:10.1128/aac.36.5.1170-a

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“…Prulifloxacin (AF3012 or NM441), a new quinolonic antibacterial agent prodrug of AF3013 (or NM394), extensively investigated in Europe and in Japan for the treatment of respiratory and urinary tract infections (11), has a wide spectrum of antibacterial activity against Gram-negative and Gram-positive strains comparable to or higher than that of other reference drugs (12,13,14).…”

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confidence: 99%

Single-Dose Prulifloxacin Versus Single-Dose Pefloxacin in the Treatment of Acute Uncomplicated Urinary Tract Infection in Women

Cervigni

Orticelli²,

Bologna

et al. 2010

UIJ

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The aim of the study was to compare the efficacy and safety of singledose prulifloxacin vs. single-dose pefloxacin in the treatment of patients with acute uncomplicated urinary tract infections. Two hundred and thirty-one female out-patients were considered microbiologically evaluable and randomly treated with 600 mg prulifloxacin (116 patients) or 800 mg pefloxacin (115 patients). The most commonly isolated uropathogen at baseline was Escherichia coli (71.4%), followed by Proteus mirabilis (10.8%) and Klebsiella pneumoniae (7.8%). Five-seven days posttreatment, the eradication rate was 97.4% and 92.2% in the prulifloxacin and pefloxacin group, respectively. The one-tailed 95% confidence interval analysis showed the equivalence of treatments. Four weeks from treatment no relapses, reinfections or superinfections were observed. The clinical success rates were 92.2% in the prulifloxacin and 84.3% pefloxacin groups. The safety profile was very good with both drugs. The results of the study make it possible to consider prulifloxacin a possible therapeutic option in patients with acute uncomplicated UTIs

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Section: Introductionmentioning

confidence: 99%

Single-Dose Prulifloxacin Versus Single-Dose Pefloxacin in the Treatment of Acute Uncomplicated Urinary Tract Infection in Women

Cervigni

Orticelli²,

Bologna

et al. 2010

UIJ

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“…In the course of our search for a new 6-fluoroquinolone antibacterial agent, thiazeto-quinoline carboxylic acid derivatives with a sulfur atom at the C-2 position were tested, and a new compound, NM394, 6-fluoro-1-methyl-7-(1-piperazinyl)-4-oxo-4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, was chosen as the most promising compound with potent antibacterial activity in vitro (7). However, despite its broad spectrum of activity, the protective effect ofNM394 against experimental infections is poor when it is administered orally.…”

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In vivo evaluation of NM441, a new thiazeto-quinoline derivative

Ozaki

Matsuda

Tomii

et al. 1991

Antimicrob Agents Chemother

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NM441 is a lipophilic prodrug of a new thiazeto-quinoline carboxylic acid derivative NM394, and when it is administered orally it is readily absorbed and hydrolyzed to its parent compound. After oral administration of NM441 at a dose of 20 mg/kg to dogs, the peak concentration of NM394 in plasma was 2.39 ,&g/ml, whereas it was 0.63 ,ug/ml for NM394 administered alone. In the course of our search for a new 6-fluoroquinolone antibacterial agent, thiazeto-quinoline carboxylic acid derivatives with a sulfur atom at the C-2 position were tested, and a new compound, NM394, 6-fluoro-1-methyl-7-(1-piperazinyl)-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, was chosen as the most promising compound with potent antibacterial activity in vitro (7). However, despite its broad spectrum of activity, the protective effect ofNM394 against experimental infections is poor when it is administered orally. In order to increase the absorption of NM394 from the intestinal tract, the prodrug of NM394, NM441, 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo -1,3 -dioxolen -4 -yl)methyl-1 -piperazinyl] -4 -oxo-4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, was synthesized ( Fig. 1). When NM441 was administered orally, it was readily absorbed and hydrolyzed to its parent compound, NM394, in blood and showed an excellent protective effect against experimental infections in mice. In this study, we compared the in vivo antibacterial activity and pharmacokinetic parameters of NM441 dosed orally compared with those of ciprofloxacin (11), ofloxacin (9) and enoxacin (4) and determined the pharmacokinetics of NM394 and NM441 in dogs.

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In Vitro Antibacterial Activity of a New Quinolone, NM394

Cited by 2 publications

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Single-Dose Prulifloxacin Versus Single-Dose Pefloxacin in the Treatment of Acute Uncomplicated Urinary Tract Infection in Women

Single-Dose Prulifloxacin Versus Single-Dose Pefloxacin in the Treatment of Acute Uncomplicated Urinary Tract Infection in Women

In vivo evaluation of NM441, a new thiazeto-quinoline derivative

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