Miyamoto, Teruyuki; Matsumoto, Junichi; Chiba, Katsumi; Egawa, Hiroshi; Shibamori, Kohichiro; Minamida, Akira; Nishimura, Yoshiro; Okada, Hidetsugu; Kataoka, Masahiro published the artcile< Pyridonecarboxylic acids as antibacterial agents. Part 14. Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency>, Reference of 22476-74-0, the main research area is cyclopropylfluoropiperazinylquinolonecarboxylate preparation bactericide; structure activity cyclopropylfluoropiperazinylquinolonecarboxylate bactericide; sparfloxacin preparation crystal structure bactericide; quinolonecarboxylic acid substituted preparation bactericide; piperazinylcyclopropylfluoroquinolonecarboxylic acid preparation bactericide.
A series of 5,7-disubstituted 1-cyclopropyl-6,8-difluoro-4-oxoquinoline-3-carboxylic acids, e.g., I (R = Cl, F, OH, NH2, SH, SMe, OMe, OCH2Ph, R1 = F, substituted piperazinyl) were prepared In vitro antibacterial screening results indicated that the amino group was optimal among the C-5 substituents. A combination of the C-5 amino group and the C-7 3,5-dimethylpiperazinyl appendage in this series conferred the best overall antibacterial property with no adverse drug interactions. I (R = NH2, R1 = cis-3,5-dimethylpiperazin-1-yl), was superior to ciprofloxacin in both in vitro and in vivo potency and hence was selected as a promising candidate for an improved therapeutic agent.
Journal of Medicinal Chemistry published new progress about Crystal structure. 22476-74-0 belongs to class piperazines, and the molecular formula is C6H12N2O, Reference of 22476-74-0.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics