Pazufloxacin
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Pazufloxacin Eigenschaften
- Schmelzpunkt:
- 269-271°C
- alpha
- D25 -88.0° (c = 0.5 in 0.05N aq NaOH)
- Siedepunkt:
- 531.5±50.0 °C(Predicted)
- Dichte
- 1.56
- storage temp.
- 2-8°C
- L?slichkeit
- Aqueous Base (Slightly, Sonicated), DMSO (Slightly, Heated), Methanol (Slightly)
- pka
- 5.05±0.40(Predicted)
- Farbe
- Off-White to Pale Yellow
- CAS Datenbank
- 127045-41-4(CAS DataBase Reference)
Sicherheit
Kennzeichnung gef?hrlicher | Xn,C,F | ||
---|---|---|---|
R-S?tze: | 20/21/22-34-11 | ||
S-S?tze: | 36/37-45-36/37/39-26-16 | ||
WGK Germany | 3 | ||
RTECS-Nr. | UU8815300 | ||
Toxizit?t | LD50 i.v. in male mice: >500 mg/kg (Todo) |
Pazufloxacin Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R20/21/22:Gesundheitssch?dlich beim Einatmen,Verschlucken und Berührung mit der Haut.R34:Verursacht Ver?tzungen.
R11:Leichtentzündlich.
S-S?tze Betriebsanweisung:
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn m?glich, dieses Etikett vorzeigen).
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S16:Von Zündquellen fernhalten - Nicht rauchen.
Beschreibung
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.Verwenden
Pazufloxacin is a potential antimicrobial and/or antiviral agent.Pharmazeutische Anwendungen
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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
1,1'-Carbonylbis-1H-imidazol
DE
Bis(1,1-dimethylethyl)malonat
Natriumazid
Ethyl 2,3,4,5-tetrafluorobenzoate
Methansulfonsure
Natriumsulfit
Trifluoressigs?ure
Paraformaldehyde
5-(Acetamido)-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide
Diphenyldiazomethane
Dimethylsulfid
Ethyl chloroformate
Ethylacetat
1,1-Dimethoxytrimethylamin
Downstream Produkte
Pazufloxacin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 190)Lieferanten
Firmenname | Telefon | Land | Produktkatalog | Edge Rate | |
---|---|---|---|---|---|
Hebei Weibang Biotechnology Co., Ltd | +8617732866630 |
bess@weibangbio.com | China | 18147 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21632 | 55 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29871 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 |
linda@hubeijusheng.com | CHINA | 28172 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 |
sales@chemdad.com | China | 39894 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 49434 | 58 |
SIMAGCHEM CORP | +86-13806087780 |
sale@simagchem.com | China | 17365 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 |
1026@dideu.com | China | 22787 | 58 |
AFINE CHEMICALS LIMITED | +86-0571-85134551 |
sales@afinechem.com | China | 15352 | 58 |
Baoji Guokang Bio-Technology Co., Ltd. | 0917-3909592 13892490616 |
gksales1@gk-bio.com | China | 9310 | 58 |
127045-41-4()Verwandte Suche:
Kresoxim-methyl
DIMETHYLAMINOPYRIDINE, POLYMER-BOUND
3-Pyridylamin
Methylsalicylat
2-Pyridylamin
N,N-Dimethylpyridin-4-amin
2-[[[[(4-Methoxy-6-methyl-1,3,5-triazin-2-yl)amino]carbonyl]amino]sulfonyl]benzoic acid methyl ester
Tribenuron methyl
Lithiumdiisopropylamid
Thiophanat-methyl
Methyl
Pazufloxacin mesilate
Brommethan
Fluor
- PAZUFLOXAXIN
- T-3761
- (s)-yclopropyl)-9-fluoro-3-methyl-7-oxo
- Pazufloxacinmyesylate
- (3S)-10-(1-AMINOCYCLOPROPYL)-9-FLUORO-2,3-DIHYDRO-3-METHYL-7-OXO-7H-PYRIDO[1,2,3-DE]-1,4-BENZOXAZINE-6-CARBOXYLIC ACID
- ALKALYL
- Pazufloxaxin mesilate
- PAZUFLOXACIN 98+%
- (S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid
- PAZUFLOXACIN (PREPARATION FOR PAZUFLOXACIN MESILATE)
- PAZUFLOXACIN(ALKALYL)
- 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo- (9CI)
- (-)-(3S)-10-(1-Aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
- 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-, (3S)- (9CI)
- 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-, (S)-
- (S)-10-(1-AMINOCYCLOPROPYL)-9-FLUORO-3-METHYL-7-OXO-3,7-DIHYDRO-2H-[1,4]OXAZINO[2,3,4-IJ]QUINOLINE-6-CARBOXYLIC ACID
- 7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 2,3-dihydro-10-(1-aminocyclopropyl)-9- fluoro-3-methyl-7-oxo-, (S)-
- Pazufloxacin318.3
- Pazufloxacine
- Pazufloxacin
- (S)-10-(1-aMinocyclopropyl)-9-fluoro-3-Methy...
- (S)-10-(1-Aminocyclopropyl)-9-Fluoro-2,3-Dihydro-3-Methyl-7-Oxo-7H-Pyrido(1,2,3-De)-1,4-Benzoxazine-6-Carboxylic Acid
- 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-, (3S)-
- Pazufloxacin USP/EP/BP
- CAS No.127045-41-4 Pazufloxacin
- 127045-41-4
- C37H63NO9
- C16H15FN2O4
- BacteriostaticAntibiotics
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- PA - PENAnalytical Standards
- Pharmacology Standards
- Antibiotics
- Chemical Structure
- Chromatography
- P
- Principle
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