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Pazufloxacin

Pazufloxacin Struktur
127045-41-4
CAS-Nr.
127045-41-4
Englisch Name:
Pazufloxacin
Synonyma:
T-3761;ALKALYL;PAZUFLOXAXIN;Pazufloxacin;Pazufloxacine;PAZUFLOXACIN 98+%;Pazufloxacin318.3;PAZUFLOXACIN(ALKALYL);Pazufloxaxin mesilate;Pazufloxacinmyesylate
CBNumber:
CB2423188
Summenformel:
C16H15FN2O4
Molgewicht:
318.3
MOL-Datei:
127045-41-4.mol

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

Downstream Produkte


Pazufloxacin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 186)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hebei Weibang Biotechnology Co., Ltd
+8617732866630
bess@weibangbio.com China 18151 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21634 55
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 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 49374 58
SIMAGCHEM CORP
+86-13806087780
sale@simagchem.com China 17365 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 22784 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 9312 58

127045-41-4()Verwandte Suche:


  • 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
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