Pefloxacin mesylate

Modify Date: 2024-01-02 19:26:25

Pefloxacin mesylate Structure
Pefloxacin mesylate structure
 Common Name Pefloxacin mesylate
CAS Number 70458-95-6 Molecular Weight 429.463
Density 1.32 g/cm3 Boiling Point 529.1ºC at 760 mmHg
Molecular Formula C18H24FN3O6S Melting Point N/A
MSDS N/A Flash Point 273.8ºC

 Use of Pefloxacin mesylate


Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)Target: DNA gyrasePefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.

 Names

Name pefloxacin mesylate
Synonym More Synonyms

 Pefloxacin mesylate Biological Activity

Description Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)Target: DNA gyrasePefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Related Catalog
References

[1]. Drlica K, et al. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92.

[2]. Hussy P, et al. Effect of 4-quinolones and novobiocin on calf thymus DNA polymerase alpha primase complex, topoisomerases I and II, and growth of mammalian lymphoblasts. Antimicrob Agents Chemother. 1986 Jun;29(6):1073-8.

 Chemical & Physical Properties

Density 1.32 g/cm3
Boiling Point 529.1ºC at 760 mmHg
Molecular Formula C18H24FN3O6S
Molecular Weight 429.463
Flash Point 273.8ºC
Exact Mass 429.136993
PSA 128.53000
LogP 2.19820
Storage condition -20°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VB2002200
CHEMICAL NAME :
3-Quinolinecarboxylic acid, 1,4-dihydro-1-ethyl-6-fluoro-7-(4-methyl-1-piperaziny l)-4-oxo-, monomethanesulfonate, dihydrate
CAS REGISTRY NUMBER :
70458-95-6
LAST UPDATED :
199009
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C17-H20-F-N3-O3.C-H4-O3-S.2H2-O
MOLECULAR WEIGHT :
465.55

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2500 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold
REFERENCE :
CHDDAT Comptes Rendus des Seances de l'Academie des Sciences, Serie D: Sciences Naturelles. (Paris, France) V.262-291, 1966-80. For publisher information, see CRASEV. Volume(issue)/page/year: 292,37,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1500 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold
REFERENCE :
CHDDAT Comptes Rendus des Seances de l'Academie des Sciences, Serie D: Sciences Naturelles. (Paris, France) V.262-291, 1966-80. For publisher information, see CRASEV. Volume(issue)/page/year: 292,37,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1 gm/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold
REFERENCE :
CHDDAT Comptes Rendus des Seances de l'Academie des Sciences, Serie D: Sciences Naturelles. (Paris, France) V.262-291, 1966-80. For publisher information, see CRASEV. Volume(issue)/page/year: 292,37,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
225 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold
REFERENCE :
CHDDAT Comptes Rendus des Seances de l'Academie des Sciences, Serie D: Sciences Naturelles. (Paris, France) V.262-291, 1966-80. For publisher information, see CRASEV. Volume(issue)/page/year: 292,37,1981

 Safety Information

Hazard Codes F,C
Risk Phrases R11
Safety Phrases 16-26-36/37/39-45
HS Code 2933599090

 Customs

HS Code 2933599090
Summary 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

EINECS 274-613-9
MFCD00865015
Pefloxacin mesylate
1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid,methanesulfonic acid
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