Title: Pazufloxacin
CAS Registry Number: 127045-41-4
CAS Name: (3
S)-10-(1-Aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7
H-pyrido[1,2,3-
de]-1,4-benzoxazine-6-carboxylic acid
Manufacturers' Codes: T-3761
Molecular Formula: C16H15FN2O4
Molecular Weight: 318.30
Percent Composition: C 60.37%, H 4.75%, F 5.97%, N 8.80%, O 20.11%
Literature References: Fluorinated quinolone. Prepn: H. Narita
et al., DE 3913245;
eidem, US 4990508 (1989, 1991 both to Toyama). Synthesis: Y. Todo
et al., Chem. Pharm. Bull. 42, 2569 (1994). Antimicrobial activity: Y. Fukuoka
et al., Antimicrob. Agents Chemother. 37, 384 (1993).
Properties: Crystals, mp 269-271.5°. [a]D25 -88.0° (c = 0.5 in 0.05
N aq NaOH). LD50 i.v. in male mice: >500 mg/kg (Todo).
Melting point: mp 269-271.5°
Optical Rotation: [a]D25 -88.0° (c = 0.5 in 0.05
N aq NaOH)
Toxicity data: LD50 i.v. in male mice: >500 mg/kg (Todo)
Derivative Type: Methanesulfonate
CAS Registry Number: 163680-77-1
Synonyms: Pazufloxacin mesylate
Manufacturers' Codes: T-3762
Molecular Formula: C16H15FN2O4.CH3SO3H
Molecular Weight: 414.41
Percent Composition: C 49.27%, H 4.62%, F 4.58%, N 6.76%, O 27.03%, S 7.74%
Properties: Colorless prisms, mp 258-259°(dec). [a]D20 -64.2° (c = 1 in 1.0
N NaOH). Soly (25°) in water >200 mg/ml.
Melting point: mp 258-259°(dec)
Optical Rotation: [a]D20 -64.2° (c = 1 in 1.0
N NaOH)
Therap-Cat: Antibacterial.
Keywords: Antibacterial (Synthetic); Quinolones and Analogs.