| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H18F2N4O3.ClH |
| Molecular Weight | 436.84 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1CCN(CC1)C2=CC3=C(C=C2F)C(=O)C(=CN3C4=NC=C(F)C=C4)C(O)=O
InChI
InChIKey=UPCHGBDAUCFDMW-UHFFFAOYSA-N
InChI=1S/C20H18F2N4O3.ClH/c1-24-4-6-25(7-5-24)17-9-16-13(8-15(17)22)19(27)14(20(28)29)11-26(16)18-3-2-12(21)10-23-18;/h2-3,8-11H,4-7H2,1H3,(H,28,29);1H
Fandofloxacin is a difluoroquinolone derivative. This compound possesses an antibacterial spectrum comparable to those of rufloxacin and ciprofloxacin in vivo. Fandofloxacin showed a rapid and nearly complete absorption, and a long residence time in the body. Because it has been reported that the in vivo antibacterial activity of Fandofloxacin is comparable or superior to other quinolones, despite the fact that its in vitro activity is significantly lower than that of the other compounds, the pharmacokinetics of this antibiotic may be responsible, at least in part, for the enhanced in vivo antibacterial activity of Fandofloxacin. Fandofloxacin is an inhibitor of bacterial DNA gyrase. The toxicities and adverse effects of Fandofloxacin observed in various toxicology studies and clinical trials were less than those of commercially available drugs. It has been in phase II clinical trial for the treatment of Urinary tract infections. However, this research has been discontinued in 2008.
CNS Activity
Originator
Approval Year
Cmax
AUC
T1/2
Funbound
Sourcing
PubMed
Sample Use Guides
Against S.pyogenes, Fandofloxacin (DW-116) (MIC50=2 mg/L; MIC90=4 mg/L) was two- or four-fold more active than rufloxacin (MIC50=8 mg/L; MIC90=8 mg/L) and it exhibited similar activity to sparfloxacin, ciprofloxacin and ofloxacin. DW-116 (MIC50=4–8 mg/L; MIC90=8–32 mg/L) was more active than rufloxacin (MIC50=4–16 mg/L; MIC90=16–32 mg/L) and less active than sparfloxacin and ciprofloxacin against S. pneumoniae and Enterococcus faecalis. Antibacterial activity of DW-116 against E. coli (MIC range 0.25–32 mg/L) was slightly inferior to that of sparfloxacin (MIC range 0.03–4 mg/L), ciprofloxacin (MIC range < 0.008–1 mg/L) and ofloxacin (MIC range 0.015–16 mg/L) and similar to that of rufloxacin (MIC range 0.25–32 mg/L).
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
