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| CAS No.: | 79660-72-3 |
|---|---|
| Name: | Fleroxacin |
| Molecular Structure: | |
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| Formula: | C17H18F3N3O3 |
| Molecular Weight: | 369.34 |
| 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; |
| EINECS: | 677-525-2 |
| Density: | 1.409 g/cm3 |
| Melting Point: | 264-266 °C |
| Boiling Point: | 535.3 °C at 760 mmHg |
| Flash Point: | 277.6 °C |
| Appearance: | white needle-like crystals |
| PSA: | 65.78000 |
| LogP: | 1.70210 |
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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, |