(R)-7-(3-Aminohexahydro-1H-azepin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
- CAS NO.:141388-76-3
- Empirical Formula: C19H21ClFN3O3
- Molecular Weight: 393.84
- MDL number: MFCD00917502
- EINECS: 604-773-0
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-10-28 16:48:35
What is (R)-7-(3-Aminohexahydro-1H-azepin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid?
Absorption
Although ocular surface concentrations are high, average systemic concentrtions after three-times daily dosing was less than 0.5 ng/mL. This indicates that besifloxacin is not appreciably absorbed into the systemic and has a very low risk of systemic side effects.
Toxicity
LD50, rat: >2000 mg/kg. The most common adverse reaction reported in 2% of patients treated with besifloxacin was conjunctival redness.
Chemical properties
Yellow to slightly yellow crystalline powder
Indications
Treatment of bacterial conjunctivitis. Bacterial isolates that are susceptible to besifloxacin include: CDC coryneform group G; Corynebacterium pseudodiphtheriticum; Corynebacterium striatum; Haemophilus influenzae; Moraxella lacunata; Staphylococcus aureus; Staphylococcus epidermidis; Staphylococcus hominis; Staphylococcus lugdunensis; Streptococcus mitis group; Streptococcus oralis; Streptococcus pneumoniae; Streptococcus salivarius*
Background
Besifloxacin is a fourth generation fluoroquinolone-type opthalmic antibiotic for the treatment of bacterial conjunctivitis. FDA approved on May 28, 2009.
Definition
ChEBI: Besifloxacin is a member of quinolines.
Pharmaceutical Applications
An amino-azepinyl quinolone formulated as a suspension for ophthalmic usage. It exhibits good antistaphylococcal activity, as well as activity against Str. pneumoniae, Enterobacteriaceae, H. influenzae and Mor. catarrhalis. It is weakly active against Corynebacterium spp. and has no useful activity against Ps. aeruginosa. After instillation into the eye, less than 0.1% of the drug reaches the plasma. It is used for bacterial conjunctivitis.
Pharmacokinetics
Besifloxacin tear concentrations were higher than MIC90 (minimum inhibitory concentration) values for common bacterial pathogens and sustained for 24 hours or longer. Mean residence time in the conjunctiva was 4.7 hours.
Metabolism
No appreciable metabolism
Properties of (R)-7-(3-Aminohexahydro-1H-azepin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Boiling point: | 607.0±55.0 °C(Predicted) |
Density | 1.469 |
storage temp. | Store at -20°C |
solubility | DMSO: Insoluble; |
pka | 6.41±0.50(Predicted) |
Water Solubility | Water: Insoluble |
Safety information for (R)-7-(3-Aminohexahydro-1H-azepin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Computed Descriptors for (R)-7-(3-Aminohexahydro-1H-azepin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
New Products
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