Pazufloxacin
Description References- Product Name
- Pazufloxacin
- CAS No.
- 127045-41-4
- Chemical Name
- Pazufloxacin
- Synonyms
- T-3761;ALKALYL;PAZUFLOXAXIN;Pazufloxacin;Pazufloxacine;PAZUFLOXACIN 98+%;Pazufloxacin318.3;PAZUFLOXACIN(ALKALYL);Pazufloxaxin mesilate;Pazufloxacinmyesylate
- CBNumber
- CB2423188
- Molecular Formula
- C16H15FN2O4
- Formula Weight
- 318.3
- MOL File
- 127045-41-4.mol
Pazufloxacin Property
- Melting point:
- 269-271°C
- alpha
- D25 -88.0° (c = 0.5 in 0.05N aq NaOH)
- Boiling point:
- 531.5±50.0 °C(Predicted)
- Density
- 1.56
- storage temp.
- 2-8°C
- solubility
- Aqueous Base (Slightly, Sonicated), DMSO (Slightly, Heated), Methanol (Slightly)
- pka
- 5.05±0.40(Predicted)
- color
- Off-White to Pale Yellow
- CAS DataBase Reference
- 127045-41-4(CAS DataBase Reference)
Safety
- Hazard Codes
- Xn,C,F
- Risk Statements
- 20/21/22-34-11
- Safety Statements
- 36/37-45-36/37/39-26-16
- WGK Germany
- 3
- RTECS
- UU8815300
- Toxicity
- LD50 i.v. in male mice: >500 mg/kg (Todo)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
N-Bromosuccinimide Price
- Product number
- 34213
- Product name
- Pazufloxacin
- Purity
- VETRANAL
- Packaging
- 25mg
- Price
- $124.8
- Updated
- 2024/03/01
- Product number
- G818
- Product name
- Pazufloxacin
- Packaging
- 100mg
- Price
- $148
- Updated
- 2021/12/16
- Product number
- API0003762
- Product name
- PAZUFLOXACIN
- Purity
- 95.00%
- Packaging
- 100MG
- Price
- $234.15
- Updated
- 2021/12/16
- Product number
- API0003762
- Product name
- PAZUFLOXACIN
- Purity
- 95.00%
- Packaging
- 1G
- Price
- $785.86
- Updated
- 2021/12/16
- Product number
- API-1098
- Product name
- Pazufloxacin
- Purity
- 98%
- Packaging
- 5g
- Price
- $410
- Updated
- 2021/12/16
Pazufloxacin Chemical Properties,Usage,Production
Description
Pazufloxacin is a fluoroquinolone with a 1-aminocyclopropyl substituent at C10 position. The presence of aminoacyl group at C-10 is a unique feature of the molecule imparting potent broad spectrum activity against gram-positive and gram-negative bacteria. This activity is based on the inhibition of bacterial DNA gyrase.
Pazufloxacin is used as an injectable antibiotic with bacterial effect against cephalosporin-resistant, carbapenem-resistance, and aminoglycoside resistant strains of bacteria. The adverse effects of pazufloxacin, such as drug-induced convulsion and hypotension are less than those of other conventional injectable fluoroquinolones.
References
[1] A. Vora, Pazufloxacin, tracked from www.japi.org on 16.07.2017
[2] Jeffrey K. Aronson, Meyler’s Side Effects of Antimicrobial Drugs, 2009
[3] Satoshi Watabe, Yoshiaki Yokoyama, Kazuyuki Nakazawa, Kimikazu Shinozaki, Rika Hiraoka, Kei Takeshita and Yukio Suzuki, Simultaneous measurement of pazufloxacin, ciprofloxacin, and levofloxacin in human serum by high-performance liquid chromatography with fluorescence detection, Journal of Chromatography B, 2010, vol. 878, 1555-1561
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)
Uses
Pazufloxacin is a potential antimicrobial and/or antiviral agent.
Uses
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%.
Pazufloxacin Preparation Products And Raw materials
Raw materials
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View Lastest Price from Pazufloxacin manufacturers
- Product
- Pazufloxacin 127045-41-4
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 500000kg
- Release date
- 2024-10-25
- Product
- Pazufloxacin 127045-41-4
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 99.9%
- Supply Ability
- 100 Tons Min
- Release date
- 2021-07-19
- Product
- Pazufloxacin 127045-41-4
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-10