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Fleroxacin

Fleroxacin structure

CAS No:
79660-72-3
Formula:
C17H18F3N3O3
Chemical Name:
Fleroxacin
Synonyms:
3-Quinolinecarboxylic acid,6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-;6,8-Difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid;Ro 23-6240;AM 833;Fleroxacin;Megalocin;Flerofloxacin;Quinodis;Ro 23-6240/000;Megalone;110158-59-3;407610-62-2
Categories:
Active Pharmaceutical Ingredients > Inhibitor Drugs

Description

Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone.Target: AntibacterialFleroxacin (Ro 23-6240; AM-833) is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of gram-negative and gram-positive bacteria. Fleroxacin is characterized pharmacokinetically by a long elimination half-life (9 to 10 h) and high concentrations in plasma (e.g., maximum concentration of 2.3 micrograms/ml after an oral dose of 200 mg) [1]. Fleroxacin is effective against Haemop

Fleroxacin is a fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria. It has a role as a topoisomerase IV inhibitor, an antibacterial drug and an EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor. It is a member of quinolines, a fluoroquinolone antibiotic, a difluorobenzene, a N-alkylpiperazine and a monocarboxylic acid.|Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone. It strongly inhibits the DNA-supercoiling activity of DNA gyrase. Fleroxacin is not an inhibitor of CYP1A2.|A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.

Fleroxacin Basic Attributes

Molecular Weight：

369.34

Exact Mass：

369.34

EC Number：

1312995-182-4

UNII：

N804LDH51K

DSSTox ID：

DTXSID1046714

ATC Code：

J - Antiinfectives for systemic use

HScode：

2933990090

Characteristics

PSA：

64.1

XLogP3：

0.24

Appearance：

white to off-white

Density：

1.4±0.1 g/cm3

Melting Point：

270 °C (decomp)

Boiling Point：

535.3±50.0 °C at 760 mmHg

Flash Point：

277.6±30.1 °C

Refractive Index：

1.568

Water Solubility：

0.1 M NaOH: soluble 10mg/mL

Storage Conditions：

2-8°C

Collision Cross Section：

189.8 Å² [M+H]+ [CCS Type: TW, Method: calibrated with Waters Major Mix]|198.8 Å² [M+Na]+ [CCS Type: TW, Method: calibrated with Waters Major Mix]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

RTECS Number：

VB1999050

Precautionary statement(s)：

P260, P264, P270, P309+P311, P405, P501

Hazard Statements：

H371

GHS Classification：

|Warning|H371 (100%): May cause damage to organs [Warning Specific target organ toxicity, single exposure]|P260, P264, P270, P309+P311, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

Drug Indication：

Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone.

Pharmacology：

Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone. It strongly inhibits the DNA-supercoiling activity of DNA gyrase.

MeSH：

Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection. (See all compounds classified as Anti-Infective Agents.)|Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II. (See all compounds classified as Topoisomerase II Inhibitors.)

Absorption：

Rapidly and well absorbed from the gastrointestinal tract after oral administration.

Mechanism of Action：

The inhibition of DNA gyrase and DNA topoisomerase 2 leads ultimately to cell death as these enzymes are required for bacterial DNA replication, transcription, repair, strand supercoiling repair, and recombination.

MeSH Entry Terms：

AM 833

Fleroxacin Use and Manufacturing

Uses

An antibacterial

Use Classification：

Pharmaceuticals

Computed Properties

Molecular Weight:369.34
XLogP3:-0.1
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:4
Exact Mass:369.13002593
Monoisotopic Mass:369.13002593
Topological Polar Surface Area:64.1
Heavy Atom Count:26
Complexity:595
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Potassium carbonate

Ethanol

Drug Function and Efficacy

This product is a quinolone antibacterial drug, which has strong antibacterial effect on Gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae, Proteus, Salmonella typhi, Salmonella paratyphi, Shigella, Enterobacter cloacae, Enterobacter aerogenes, Citrobacter, Serratia marcescens, Pseudomonas aeruginosa, Neisseria meningitidis, Haemophilus influenzae, Moracata, Legionella pneumophila, Neisseria gonorrhoeae, etc. It also has moderate antibacterial effect on Gram-positive cocci such as Staphylococcus and hemolytic Streptococcus. The mechanism of action of this product is to inhibit the bacterial DNA gyrase and thus kill the bacteria.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Fleroxacin and Glucose Injection
Ingredients	The main ingredient of this product is fleroxacin.
Indication	1. The aluminum and magnesium contained in didanosine (DDI) preparations can chelate with fluoroquinolones and should not be used together. 2. Urine alkalinizers can reduce the solubility of this product in urine, leading to crystalluria and nephrotoxicity. 3. Probenecid can delay the excretion of this product, increase the blood concentration of this product and produce toxicity.
Specifications	100ml: Fleroxacin 0.2g and glucose 5g

Fleroxacin and Glucose Injection
Ingredients	The main ingredient of this product is fleroxacin
Indication	The aluminum and magnesium contained in didanosine (DDI) preparations can chelate with fluoroquinolones and should not be used together. Urine alkalinizers can reduce the solubility of this product in urine, leading to crystalluria and nephrotoxicity. 3. Probenecid can delay the excretion of this product, increase the blood concentration of this product and produce toxicity.
Specifications	100ml: Fleroxacin 0.2g and glucose 5.0g

Fleroxacin and Glucose Injection
Ingredients	The main ingredient of this product is fleroxacin.
Indication	1. The aluminum and magnesium contained in didanosine (DDI) preparations can chelate with fluoroquinolones and should not be used together. 2. Urine alkalinizers can reduce the solubility of this product in urine, leading to crystalluria and nephrotoxicity. 3. Probenecid can delay the excretion of this product, increase the blood concentration of this product and produce toxicity.
Specifications	100ml: Fleroxacin 0.2g and glucose 5.0g

See More Related Drugs

Registered Holders

Qingdao Shouhejinhai Pharmaceutical Ltd.

China
Active
Zhengzhou Ruikang Pharmaceutical Co., Ltd.

China
Active
Henan Kangtai Pharmaceutical Co., Ltd.

China
Active

See More Registered Holders

Recommended Suppliers of Fleroxacin

Shandong Airuike Chemical Co., Ltd. Contact Supplier

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Fleroxacin CAS79660-72-3 White to yellowish crystalline powder

CAS No.: 79660-72-3

Grade: Pharmaceutical grade

Content: 99%

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HANGZHOU LEAP CHEM CO., LTD. Contact Supplier

CN
5 YRS

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Fleroxacin

CAS No.: 79660-72-3

Content: 99.00%

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