Title: Sparfloxacin
CAS Registry Number: 110871-86-8
CAS Name: rel-5-Amino-1-cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Manufacturers' Codes: AT-4140; CI-978; PD-131501
Trademarks: Spara (Dainippon); Zagam (Specia)
Molecular Formula: C19H22F2N4O3
Molecular Weight: 392.40
Percent Composition: C 58.16%, H 5.65%, F 9.68%, N 14.28%, O 12.23%
Literature References: Fluorinated quinolone antibacterial. Prepn: J. Matsumoto et al., EP 221463; eidem, US 4795751 (1987, 1989 both to Dainippon). Synthesis and structure-activity relationship: T. Miyamoto et al., J. Med. Chem. 33, 1645 (1990). Antibacterial activity: S. Nakamura et al., Antimicrob. Agents Chemother. 33, 1167 (1989). Comparative in vitro antimicrobial spectrum: T. Kojima et al., ibid. 1980. Pharmacokinetics: S. Nakamura et al., ibid. 34, 89 (1990). Subacute toxicity studies: M. Yasuba et al., Chemotherapy 39, Suppl. 4, 180 (1991), C.A. 115, 247561d (1991); M. Iida et al., ibid. 195, C.A. 115, 247562e (1991).
Properties: Crystals from chloroform + ethanol, mp 266-269° (dec). pKa1 6.25, pKa2 9.30.
Melting point: mp 266-269° (dec)
pKa: pKa1 6.25, pKa2 9.30
Therap-Cat: Antibacterial.
Keywords: Antibacterial (Synthetic); Quinolones and Analogs. |