Title: Rufloxacin
CAS Registry Number: 101363-10-4
CAS Name: 9-Fluoro-2,3-dihydro-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzothiazine-6-carboxylic acid
Manufacturers' Codes: MF-934
Molecular Formula: C17H18FN3O3S
Molecular Weight: 363.41
Percent Composition: C 56.18%, H 4.99%, F 5.23%, N 11.56%, O 13.21%, S 8.82%
Literature References: Fluorinated quinolone; structurally similar to ofloxacin, q.v. Prepn: G. Mascellani et al., AU 85 39142; eidem, US 4684647 (1985, 1987 both to Mediolanum); V. Cecchetti et al., J. Med. Chem. 30, 465 (1987). In vitro activity: R. Wise et al., Antimicrob. Agents Chemother. 29, 649 (1992). Mechanism of action and resistance: L. J. V. Piddock et al., J. Antimicrob. Chemother. 31, 855 (1993). Pharmacokinetics and safety: J. C. Kisicki et al., ibid. 36, 1296 (1992). HPLC determn in biological fluids: F. Lombardi et al., J. Chromatogr. 576, 129 (1992). Clinical study in cystitis and urinary tract infections: R. Mattina et al., Infection 21, 106 (1993); in bronchitis: W. Klietmann et al., Antimicrob. Agents Chemother. 37, 2298 (1993).
Derivative Type: Hydrochloride
CAS Registry Number: 106017-08-7
Manufacturers' Codes: ISF-09334
Trademarks: Qari (Mediolanum); Monos (SKB); Tebraxin (Bracco)
Molecular Formula: C17H18FN3O3S.HCl
Molecular Weight: 399.87
Percent Composition: C 51.06%, H 4.79%, F 4.75%, N 10.51%, O 12.00%, S 8.02%, Cl 8.87%
Properties: Crystals from ethanol/water, mp 322-324° (Cecchetti). LD50 in rats, mice (mg/kg): 285, 224 i.v.; LD50 in rabbits, male, female rats (mg/kg): 660, 631, 501 orally (Cecchetti).
Melting point: mp 322-324° (Cecchetti)
Toxicity data: LD50 in rats, mice (mg/kg): 285, 224 i.v.; LD50 in rabbits, male, female rats (mg/kg): 660, 631, 501 orally (Cecchetti)
Therap-Cat: Antibacterial.
Keywords: Antibacterial (Synthetic); Quinolones and Analogs. |