Temafloxacin (hydrochloride)
MIC90: less than or equal to 0.06 micrograms/mL respiratory pathogens
Temafloxacin is a fluoroquinolone antibiotic.
Fluoroquinolone antibiotic is an organonitrogen heterocyclic antibiotic with a quinolone or quinolone-like moiety and have a fluorine atom attached to the central ring system.
In vitro: The in-vitro activities of temafloxacin, ciprofloxacin, and ofloxacin against gram-negative bacteria were compared. The 90% minimal inhibitory concentrations (MIC90s) of temafloxacin for respiratory pathogens were less than or equal to 0.06 micrograms/mL. Temafloxacin was also active against bacterial agents of sexually transmitted diseases, such as Neisseria gonorrhoeae and Chlamydia trachomatis [1].
In vivo: Mixed aerobic-anaerobic infection was induced by i.p. implantation of gelatin capsules containing Bacteroides fragilis, Escherichia coli, and sterile rat faeces. Temafloxacin was found to be highly active with a 90.9% cure rate in comparison with no treatment, and as active as a combination of clindamycin and gentamicin. Temafloxacin at 12 mg/dose resulted in rise to serum concentrations exceeding the MIC values of both microorganisms for at least 8 h [2].
Clinical trial: Clinical studies showed that temafloxacin has improved activity against pneumococci. Eradication rates in acute exacerbations of chronic bronchitis collated from individual studies are 98% overall and 100% in pneumococcal infections. Moreover, eradication rates in smokers and the elderly illustrate significant advantages for temafloxacin. In pneumonia, a twice-daily temafloxacin regimen has given equivalent overall results to those of amoxycillin (84.6% vs 80%) [3].
References:
[1] Hardy DJ. In vitro activity of temafloxacin against gram-negative bacteria: an overview. Am J Med. 1991 Dec 30;91(6A):19S-23S.
[2] Thadepalli H, Hajji M, Perumal VK, Chuah SK, Gollapudi S. Evaluation of temafloxacin in a rat model of intra-abdominal abscess. J Antimicrob Chemother. 1992 Jun;29(6):687-92.
[3] Ball P. The role of temafloxacin in the community setting: an overview. J Antimicrob Chemother. 1991 Dec;28 Suppl C:121-30.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 453.8 |
| Cas No. | 105784-61-0 |
| Formula | C21H18F3N3O3·HCl |
| Synonyms | A-62254 |
| Solubility | ≤2mg/ml in DMSO;5mg/ml in dimethyl formamide |
| Chemical Name | 1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, monohydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC1CN(C2=C(F)C=C(C(C(C(O)=O)=CN3C4=CC=C(F)C=C4F)=O)C3=C2)CCN1.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
|
Cell lines |
H.influenzae, Moraxella Catarrhalis, Bordetella pertussis, Bordetella Parapertussis, N.meningitidis |
|
Preparation method |
The solubility of this compound in DMSO is ≤ 2mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
0～2 μg/ml |
|
Applications |
The 90% minimal inhibitory concentration of temafloxacin against respiratory pathogens such as Haemophilus influenzae, Moraxella catarrhalis, Neisseria meningitidis, Bordetella pertussis, and Legionella pneumophila is (MIC90s) ≤ 0.06 μg / mL. Temafloxacin also has resistance to bacteria of sexually transmitted diseases, including Neisseria gonorrhoeae (MIC90≤0.015μg/mL) and Chlamydia trachomatis (MIC90 0.25μg/mL). |
| Animal experiment [1]: | |
|
Animal models |
Intra-abdominal abscess model in rats |
|
Dosage form |
12 mg/dose |
|
Application |
Compared with untreated, temafloxacin was found to have high activity with a cure rate of 90.9%, and was comparable to the combined activity of clindamycin and gentamicin. Temafloxacin at 12mg/dose caused an increase in serum concentration, exceeding the MIC values of the two microorganisms for at least 8 hours. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Hardy DJ. In vitro activity of temafloxacin against gram-negative bacteria: an overview. Am J Med. 1991 Dec 30;91(6A):19S-23S. doi: 10.1016/0002-9343(91)90304-g. PMID: 1662890. [2]. Thadepalli H, Hajji M, Perumal VK, Chuah SK, Gollapudi S. Evaluation of temafloxacin in a rat model of intra-abdominal abscess. J Antimicrob Chemother. 1992 Jun;29(6):687-92. doi: 10.1093/jac/29.6.687. PMID: 1324241. |
|
Quality Control & MSDS
- View current batch:
-
Purity ≥ 95.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
