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119354-43-7

119354-43-7 structure
119354-43-7 structure
  • Name: Antofloxacin
  • Chemical Name: (S)-Antofloxacin
  • CAS Number: 119354-43-7
  • Molecular Formula: C18H21FN4O4
  • Molecular Weight: 376.38200
  • Catalog: Signaling Pathways Anti-infection Bacterial
  • Create Date: 2017-08-09 07:42:07
  • Modify Date: 2025-08-25 18:15:13
  • Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species[1][2][3].

Name (S)-Antofloxacin
Synonyms 7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid,8-amino-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-,(3S)
UNII-56A192VX1Q
Antofloxacin
Description Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species[1][2][3].
Related Catalog
Target

Bacterial[1][2]

In Vivo Antofloxacin (2.5~160 mg/kg; s.c.; 24 hours) penetration ratio ranges from 1.22 to 1.54 for the total drug concentrations and is independent of the dose levels[3].Antofloxacin increases the plasma theophylline concentration, partly by acting as a mechanism based inhibitor of CYP1A2. Antofloxacin inhibits the formation of the three metabolites of theophylline was time-, concentration- and NADPH-dependent, which is characteristic of mechanism-based inhibition[2]. Animal Model: Mice[3] Dosage: 2.5~160 mg/kg (Pharmacokinetic Analysis) Administration: S.c.; 24 hours Result: Penetration ratio ranged from 1.22 to 1.54 for the total drug concentrations and was independent of the dose levels.
References

[1]. He XJ, et al. Efficacy and Safety of Antofloxacin-Based Triple Therapy for Helicobacter pylori Eradication Failure in China [published online ahead of print, 2021 Feb 8]. Dig Dis Sci. 2021;10.1007/s10620-021-06856-z.

[2]. Liu L, et al. Modulation of pharmacokinetics of theophylline by antofloxacin, a novel 8-amino-fluoroquinolone, in humans. Acta Pharmacol Sin. 2011;32(10):1285-1293.

[3]. Zhou YF, et al. In Vivo Pharmacokinetic and Pharmacodynamic Profiles of Antofloxacin against Klebsiella pneumoniae in a Neutropenic Murine Lung Infection Model. Antimicrob Agents Chemother. 2017;61(5):e02691-16. Published 2017 Apr 24.

Molecular Formula C18H21FN4O4
Molecular Weight 376.38200
Exact Mass 376.15500
PSA 101.03000
LogP 1.71030
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