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Sitafloxacin

Names

[ CAS No. ]:
163253-37-0

[ Name ]:
Sitafloxacin

[Synonym ]:
Sitafloxacin hydrate
7-[(7S)-7-Amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid hydrate (1:1)
Spifloxacin hydrate
UNII-45IP57B62B
Gracevit
3-Quinolinecarboxylic acid, 7-[(7S)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-, hydrate (1:1)
Sitafloxacin

Biological Activity

[Description]:

Sitafloxacin (DU6859a) monohydrate is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin monohydrate shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin monohydrate can be used for the research of respiratory tract infection and urinary tract infection[1][2].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Sitafloxacin (DU6859a) monohydrate shows antibacterial activities with MIC of 0.03, 0.12, 0.06 mg/L for wild-type ATCC 49619, gyrA mutant SP39, parC mutant 1026523 streptococcus pneumoniae stran, respectively[1]. Sitafloxacin (DU6859a) monohydrate shows antibacterial activities for quinolone-susceptible strains of streptococcus pneumoniae with MIC of 0.03, 0.03 mg/L for EG 00093 and EG 00218 strain, respectively[1]. Sitafloxacin (DU6859a) monohydrate shows inhibition for DNA gyrase and topoisomerase IV (TopoIV) with >IC50s of 4.38, 3.12 mg/L, respectively[1].

[In Vivo]

Sitafloxacin (DU6859a; 12.5-100 mg/kg; i.g.; daily for 4 weeks; BALB/c female mice) monohydrate has antibacterial activity. M. ulcerans cells could be isolated from the inoculated footpads and there was no evidence of footpad swelling[2]. Animal Model: BALB/c female mice[2] Dosage: 12.5, 25, 50 and 100 mg/kg Administration: Oral gavage; daily, for 4 weeks Result: Inhibits the growth of Mycobacterium ulcerans and the M. ulcerans cells.

[References]

[1]. Okumura R, et al. Dual-targeting properties of the 3-aminopyrrolidyl quinolones, DC-159a and sitafloxacin, against DNA gyrase and topoisomerase IV: contribution to reducing in vitro emergence of quinolone-resistant Streptococcus pneumoniae. J Antimicrob Chemother. 2008 Jul;62(1):98-104.

[2]. Dhople AM, et al. Activities of sitafloxacin (DU-6859a), either singly or in combination with rifampin, against Mycobacterium ulcerans infection in mice. J Chemother. 2003 Feb;15(1):47-52.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H18ClF2N3O3

[ Molecular Weight ]:
409.81400

[ Exact Mass ]:
409.10000

[ PSA ]:
88.56000

[ LogP ]:
3.46790

Related Compounds