Pazufloxacin

ChemicalBook > CAS DataBase List > 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%.

Pazufloxacin Preparation Products And Raw materials

Raw materials

1,1'-Carbonyldiimidazole DE Di-tert-Butyl malonate Sodium azide Ethyl 2,3,4,5-tetrafluorobenzoate Methanesulfonic acid Sodium sulfite Trifluoroacetic acid Paraformaldehyde 5-(Acetamido)-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide Diphenyldiazomethane Dimethyl sulfide Ethyl chloroformate Ethyl acetate N,N-Dimethylformamide dimethyl acetal

Preparation Products

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Pazufloxacin Suppliers

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View Lastest Price from Pazufloxacin manufacturers

Hebei Guanlang 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: 2022-09-30

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:

Methyl salicylate 2-Aminopyridine 4-Dimethylaminopyridine Tribenuron methyl Lithium diisopropylamide Thiophanate-methyl METSULFURON METHYL DIMETHYLAMINOPYRIDINE, POLYMER-BOUND Kresoxim-methyl 3-Aminopyridine Balofloxacin TROVAFLOXACIN Sparfloxacin Tosufloxacin Clinafloxacin Sparfloxacin Methyl 3'-FLUORO-4'-METHYLACETOPHENONE

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

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