Fleroxacin
Fleroxacin is a fluoroquinolone antibiotic that displays antibacterial activity against gram positive and gram negative bacteria. Fleroxacin inhibits bacterial DNA gyrase and helicase. In vitro, fleroxacin inhibits DNA unwinding and ATPase activities of Bloom helicase, stabilizing the enzyme in a low activity conformation, disrupting ATP hydrolysis and blocking helicase translocation on DNA strands. Additionally, fleroxacin increases reactive oxygen species (ROS) and peroxidation of squalene when exposed to UVA light, indicating phototoxicity in vitro.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18923667
| Cas No. |
79660-72-3 |
|---|---|
| Purity |
≥98% |
| Formula |
C17H18F3N3O3 |
| Formula Wt. |
369.34 |
| Chemical Name |
AM-833; Megalocin; Megalone; Quinodis |
| IUPAC Name |
6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid |
| Synonym |
AM-833; Megalocin; Megalone; Quinodis |
| Melting Point |
264-266°C |
| Solubility |
Soluble in acid, alkali, not soluble in water |
| Appearance |
White Powder |
Luo H, Xu HQ, Chen X, et al. Potent in vitro interference of fleroxacin in DNA-binding, unwinding and ATPase activities of Bloom helicase. Biomed Environ Sci. 2013 Apr;26(4):231-42. PMID: 23534463.
Kawada A, Hatanaka K, Gomi H, et al. In vitro phototoxicity of new quinolones: production of active oxygen species and photosensitized lipid peroxidation. Photodermatol Photoimmunol Photomed. 1999 Dec;15(6):226-30. PMID: 10599972
Gocke E. Mechanism of quinolone mutagenicity in bacteria. Mutat Res. 1991 May;248(1):135-43. PMID: 1851537.
