Description References
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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
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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)
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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)
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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.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
34213
Product name
Pazufloxacin
Purity
VETRANAL
Packaging
25mg
Price
$124.8
Updated
2024/03/01
AK Scientific
Product number
G818
Product name
Pazufloxacin
Packaging
100mg
Price
$148
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0003762
Product name
PAZUFLOXACIN
Purity
95.00%
Packaging
100MG
Price
$234.15
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0003762
Product name
PAZUFLOXACIN
Purity
95.00%
Packaging
1G
Price
$785.86
Updated
2021/12/16
AHH
Product number
API-1098
Product name
Pazufloxacin
Purity
98%
Packaging
5g
Price
$410
Updated
2021/12/16
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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%.

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Pazufloxacin Suppliers

J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15839
Advantage
69
TAIYUAN RHF CO.,LTD.
Tel
+86 351 7031519
Fax
+86 351 7031519
Email
sales@RHFChem.com
Country
China
ProdList
2338
Advantage
56
Pure Chemistry Scientific Inc.
Tel
001-857-928-2050 or 1-888-588-9418
Fax
001-617-206-9595
Email
sales@chemreagents.com
Country
United States
ProdList
10186
Advantage
62
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202 13764082696
Email
info@hanhongsci.com
Country
China
ProdList
42958
Advantage
64
XiaoGan ShenYuan ChemPharm co,ltd
Tel
15527768850
Email
1791901229@qq.com
Country
China
ProdList
8836
Advantage
52
Sichuan Kulinan Technology Co., Ltd
Tel
400-1166-196 18981987031
Fax
028-84555506 800101999
Email
cdhxsj@163.com
Country
China
ProdList
11707
Advantage
57
Tianjin heowns Biochemical Technology Co., Ltd.
Tel
400 638 7771
Email
sales@heowns.com
Country
China
ProdList
14435
Advantage
57
Shanghai T&W Pharmaceutical Co., Ltd.
Tel
+86 21 61551611
Fax
+86 21 50676805
Country
China
ProdList
9891
Advantage
58
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3239
Advantage
55
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View Lastest Price from Pazufloxacin manufacturers

Hebei Weibang Biotechnology Co., Ltd
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
Dideu Industries Group Limited
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
Zhuozhou Wenxi import and Export Co., Ltd
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

127045-41-4, PazufloxacinRelated Search:


  • 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
  • (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
  • Pazufloxacin
  • (S)-10-(1-aMinocyclopropyl)-9-fluoro-3-Methy...
  • 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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