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
- Molecular Weight:
- 318.3
- MOL File:
- 127045-41-4.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/5/18 11:31:07
| 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
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302+H312+H332 |
| Precautionary statements | P261-P264-P280-P301+P312-P302+P352+P312-P304+P340+P312 |
| 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) |
Pazufloxacin Chemical Properties,Uses,Production
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.
Uses
Pazufloxacin is a potential antimicrobial and/or antiviral agent.
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
1of3
chevron_rightPreparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Uni Trade Agencies | 08068442234Ext 578 | Mumbai, India | 10 | 58 | Inquiry |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | China | 21662 | 55 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29899 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49403 | 58 | Inquiry |
| SIMAGCHEM CORP | +86-13806087780 | China | 17367 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 23430 | 58 | Inquiry |
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | China | 15372 | 58 | Inquiry |
| Baoji Guokang Bio-Technology Co., Ltd. | 0917-3909592 13892490616 | China | 9316 | 58 | Inquiry |