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HomeProduct name listPazufloxacin

Pazufloxacin

  • CAS NO.:127045-41-4
  • Empirical Formula: C16H15FN2O4
  • Molecular Weight: 318.3
  • MDL number: MFCD00865012
  • EINECS: 635-036-1
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-10-25 23:13:37
Pazufloxacin Structural

What is Pazufloxacin?

Description

Pazufloxacin is a novel quinolone marketed for the treatment of bacterial infections in Japan. This tricyclic fluoro-quinolone can be synthesized in 11 steps from commercially available 2,3,4,5tetrafluorobenzoic acid. The cyclopropyl substituent is first introduced in 6 steps including 4-F-substitution with tert-butylcyanoacetate, decarboxylation, aa alkylation with 1 ,Zdibromoethane, partial nitrile hydrolysis and Hoffmann-rearrangement. The pyridoxazine ring is then introduced in 5 steps including 6-ketoester formation and pryridoxazine annulation. Pazufloxacin displays a broad spectrum activity against Grampositive and Gram-negative bacteria, although it is less active that ciprofloxacin against pneumococci and is not active against ciprofloxacin-resistant isolates. In patients with gonococcal urethritis a high prevalence of fluoroquinolone-resistant N. gonorrhoeae isolates with the Ser-91-to-Phe mutation in GyrA was observed. However, good clinical responses have been seen in clinical trials of patients with urinary tract infections and to a lesser extent with respiratory tract infections. Pazufloxacin is mainly excreted in urine with a short half-life (2-2.5 h). It has a phototoxicity equal to that of ciprofloxacin and its adverse effect profile resembles that of other quinolones.

Originator

Toyama (Japan)

The Uses of Pazufloxacin

Pazufloxacin is a potential antimicrobial and/or antiviral agent.

The Uses of Pazufloxacin

antibactierial

Definition

ChEBI: LSM-5745 is a member of quinolines.

brand name

Pasil, Pazucross

Pharmaceutical Applications

A tricyclic fluoroquinolone, formulated as mesylate and hydrochloride salts for oral or parenteral use or as a methane sulfonate (eye ointment).
It displays good activity in vitro against methicillin susceptible Staph. aureus (MIC 0.2 mg/L), but is inactive against Str. pyogenes, Str. pneumoniae (MIC ≥4 mg/L) and enterococci. L. pneumophila is inhibited by 0.03 mg/L. Activity against Enterobacteriaceae, fastidious Gram-negative bacilli, Ps. aeruginosa and Acinetobacter spp. is similar to that of ofloxacin. It is weakly active against Sten. maltophilia and Burkholderia cepacia (MIC c. 2 mg/L). Against M. tuberculosis, MICs range from 0.8 to 4 mg/L. It is inactive against anaerobes.
After oral doses of 100 or 400 mg, peak plasma concentrations range from 0.94 mg/L (100 mg) to 4.5 mg/L (400 mg) after <1 h. The apparent elimination half-life is around 2 h. Most of the administered dose is eliminated in urine, about 70% within 24 h. Four metabolites have been reported. In elderly patients, according to the renal function, the peak plasma concentration may be elevated (up to 5.6 mg/L) and significantly delayed (2–6 h). The plasma protein binding ranges from 17% to 28%.

Properties of Pazufloxacin

Melting point: 269-271°C
Boiling point: 531.5±50.0 °C(Predicted)
alpha  D25 -88.0° (c = 0.5 in 0.05N aq NaOH)
Density  1.56
storage temp.  2-8°C
solubility  Aqueous Base (Slightly, Sonicated), DMSO (Slightly, Heated), Methanol (Slightly,
form  neat
pka 5.05±0.40(Predicted)
color  Off-White to Pale Yellow
CAS DataBase Reference 127045-41-4(CAS DataBase Reference)

Safety information for Pazufloxacin

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

Computed Descriptors for Pazufloxacin

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