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Fleroxacin

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Name

Fleroxacin

EINECS 677-525-2
CAS No. 79660-72-3 Density 1.409 g/cm3
PSA 65.78000 LogP 1.70210
Solubility N/A Melting Point 264-266 °C
Formula C17H18F3N3O3 Boiling Point 535.3 °C at 760 mmHg
Molecular Weight 369.34 Flash Point 277.6 °C
Transport Information N/A Appearance white needle-like crystals
Safety Risk Codes N/A
Molecular Structure Molecular Structure of 79660-72-3 (Fleroxacin) Hazard Symbols N/A
Synonyms

Fleroxacin [USAN:BAN:INN:JAN];Ro 23-6240;FLRX;Megalocin (TN);AM 833;3-Quinolinecarboxylic acid, 1,4-dihydro-6,8-difluoro-1-(2-fluoroethyl)-7-(4-methyl-1-piperazinyl)-4-oxo-;Fleroxicin;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;Megalone;Fleroxacine [French];Fleroxacin (JAN/USAN);Fleroxacinum [Latin];Megalone (TN);Fleroxacino [Spanish];Megalocin;Fleroxacin Hydrochloride;

Article Data 5

Fleroxacin Specification

The Fleroxacin , its cas register number is 79660-72-3. The IPUAC name about this chemicals is 6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid . The enthalpy of vaporization about it is 85.44 kJ/mol, vapour pressure is 2.73E-12 mmHg at 25°C. Product categories about this chemicals are Antibiotics for Research and Experimental Use; Biochemistry; Quinolones (Antibiotics for Research and Experimental Use); Intermediates & Fine Chemicals; Pharmaceuticals .

The Fleroxacin is sold under the brand names Quinodis and Megalocin. It has good activity against a wide range of Gram-positive and Gram-negative bacteria. Endothal is a broad-spectrum antimicrobial fluoroquinolone. It has good activity against infection such as colibacillus, genus Proteus, Klebsiella pneumoniae and so on. As a safe and effective fluoroquinolone antibiotic, Fleroxacin is similar to ciprofloxacin. It strongly inhibits the DNA-supercoiling activity of DNA gyrase. Fleroxacin are able to kill bacteria by inhibiting activity of RNA.

Treatments with with oral and intravenous fleroxacin are safe in clinical trials. It may cause insomnia, adverse reactions involved gastrointestinal tract and the central nervous system, but most of adverse effects were of mild intensity and reversible. The most frequently reported events were insomnia, headache, dizziness, and digestive system disorders. More fleroxacin-treated patients experienced phototoxicity and treatment-limiting adverse events.

This chemicals can be described computed from structure:
1) SMILES: CN1CCN(CC1)C2=C(C=C3C(=C2F)N(C=C(C3=O)C(=O)O)CCF)F
2) InChI:  InChI=1S/C17H18F3N3O3/c1-21-4-6-22(7-5-21)15-12(19)8-10-14(13(15)20)23(3-2-18)9-11(16(10)24)17(25)26/h8-9H,2-7H2,1H3,(H,25,26)

The most important thing about Fleroxacin is the toxicity, following is the form:

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
dog LD50 oral > 1gm/kg (1000mg/kg) GASTROINTESTINAL: NAUSEA OR VOMITING

MUSCULOSKELETAL: JOINTS
Chemotherapy Vol. 38(Suppl,
mouse LD50 intraperitoneal > 1500mg/kg (1500mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
Chemotherapy Vol. 38(Suppl,
mouse LD50 intravenous 21730ug/kg (21.73mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
Chemotherapy Vol. 38(Suppl,
mouse LD50 oral > 4gm/kg (4000mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
Chemotherapy Vol. 38(Suppl,
mouse LD50 subcutaneous > 1500mg/kg (1500mg/kg)   Chemotherapy Vol. 38(Suppl,
rat LD50 intraperitoneal > 1500mg/kg (1500mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
Chemotherapy Vol. 38(Suppl,
rat LD50 intravenous 20405ug/kg (20.405mg/kg) SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)
Chemotherapy Vol. 38(Suppl,
rat LD50 oral > 4gm/kg (4000mg/kg)   Chemotherapy Vol. 38(Suppl,
rat LD50 subcutaneous > 1500mg/kg (1500mg/kg) SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE" Chemotherapy Vol. 38(Suppl,

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