Pazufloxacin

Bezeichnung:Pazufloxacin

CAS-Nr127045-41-4

Englisch Name:Pazufloxacin

CBNumberCB2423188

SummenformelC16H15FN2O4

Molgewicht318.3

MOL-Datei127045-41-4.mol

Pazufloxacin physikalisch-chemischer 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
Löslichkeit	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 gefährlicher	Xn,C,F
R-Sätze:	20/21/22-34-11
S-Sätze:	36/37-45-36/37/39-26-16
WGK Germany	3
RTECS-Nr.	UU8815300
Toxizität	LD50 i.v. in male mice: >500 mg/kg (Todo)

Gefahreninformationscode (GHS)

Pazufloxacin Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
R34:Verursacht Verätzungen.
R11:Leichtentzündlich.
S-Sätze Betriebsanweisung:
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, 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.
Originator
Toyama (Japan)
Verwenden
Pazufloxacin is a potential antimicrobial and/or antiviral agent.
Verwenden
antibactierial
Definition
ChEBI: LSM-5745 is a member of quinolines.
Trademarks
Pasil, Pazucross
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

Pazufloxacin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

127045-41-4, Pazufloxacin Verwandte Suche:

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