Prulifloxacin

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Names

[ Name ]:
Prulifloxacin

[Synonym ]:
SEA BUCKTHORN P.E
6-Fluoro-1-methyl-7-{4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl}-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
(±)-6-fluoro-1-methyl-7-(4-((5-methyl-2-oxo-1,3-dioxol-4-yl)methyl)-1-piperazinyl)-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic Acid
Quisnon
1H,4H-[1,3]Thiazeto[3,2-a]quinoline-3-carboxylic acid, 6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-
Prulifloxacin
6-fluoro-1-methyl-7-{4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]piperazin-1-yl}-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
(1R)-6-Fluoro-1-methyl-7-{4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl}-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
nm441
Sword
UNII:J42298IESW
(±)-7-[4-[(Z)-2,3-Dihydroxy-2-butenyl]-1-piperazinyl]-6-fluoro-1-methyl-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic Acid Cyclic Carbonate
(1R)-6-fluoro-1-methyl-7-{4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]piperazin-1-yl}-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
1H,4H-[1,3]Thiazeto[3,2-a]quinoline-3-carboxylic acid, 6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-, (1R)-
MFCD00864847

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
633.2±65.0 °C at 760 mmHg

[ Melting Point ]:
211-214°C

[ Molecular Formula ]:
C₂₁H₂₀FN₃O₆S

[ Molecular Weight ]:
461.463

[ Flash Point ]:
336.8±34.3 °C

[ Exact Mass ]:
461.105682

[ PSA ]:
134.43000

[ LogP ]:
3.27

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.721

[ Storage condition ]:
-20°C Freezer

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ0600000

CHEMICAL NAME :: 1H,4H-(1,3)Thiazeto(3,2-a)quinoline-3-carboxylic acid, 6-fluoro-1-methyl-7-(4-((5-methyl-2- oxo-1,3-dioxol-4-yl)methyl)-1-piperazinyl)-4-oxo-

CAS REGISTRY NUMBER :: 123447-62-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C21-H20-F-N3-O6-S

MOLECULAR WEIGHT :: 461.50

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),33,1996

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 915 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),33,1996

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),33,1996

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 35,4727,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1652 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Skin and Appendages - hair

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),33,1996

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),33,1996

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),149,1996 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8400 mg/kg/4W-I

TOXIC EFFECTS :: Gastrointestinal - other changes Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in sodium

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),45,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 gm/kg/13W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),89,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 21 gm/kg/4W-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in leukocyte (WBC) count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),71,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 45500 mg/kg/13W-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Blood - change in clotting factors Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 21(Suppl 1),113,1996

Safety Information

[ Hazard Codes ]:
Xi

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

4-(Bromomethyl)-5-methyl-1,3-dioxol-2-one
UNII:C38638H76Y
Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate
3,4-Difluorophenyl isothiocyanate
triethylammonium (3,4-difluorophenyl)dithiocarbamate
3,4-Difluoroaniline
6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid acetonitrile solvate
6,7-Difluoro-4-hydroxy-2-mercaptoquinoline-3-carboxylicacidethylester
Ethyl 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate
ethyl 6,7-difluoro-4-hydroxy-2-[(methoxymethyl)thio]-quinoline-3-carboxylate

DownStream

Related Compounds

Prulifloxacin
Prulifloxacin-d8
PRULIFLOXACIN INTERMEDIATE 2
Prulifloxacin InterMediate PL-7
Prulifloxacin InterMediate PL-7
methyl 3-(3-methoxyphenyl)-2-methyl-4-oxo-3,4,5,6-tetrahydro-2H-2,6-methanobenzo[g][1,3,5]oxadiazocine-8-carboxylate
methyl 3-(3,4-dimethoxyphenyl)-2-methyl-4-oxo-3,4,5,6-tetrahydro-2H-2,6-methanobenzo[g][1,3,5]oxadiazocine-8-carboxylate
2-(3'-(3-fluorophenyl)-5-methyl-2,4'-dioxospiro[indoline-3,2'-thiazolidin]-1-yl)-N-(2-methoxyphenyl)acetamide
2-[3'-(4-fluorophenyl)-5-methyl-2,4'-dioxo-1,2-dihydrospiro[indole-3,2'-[1,3]thiazolidine]-1-yl]-N-(2-methoxyphenyl)acetamide
1-(3,4-dimethoxyphenyl)-3-((2-methylbenzyl)thio)pyrazin-2(1H)-one
3-((2-chlorobenzyl)thio)-1-(3,4-dimethoxyphenyl)pyrazin-2(1H)-one
3-((4-chlorobenzyl)thio)-1-(3,4-dimethoxyphenyl)pyrazin-2(1H)-one
3-((3-chlorobenzyl)thio)-1-(3,4-dimethoxyphenyl)pyrazin-2(1H)-one
N-benzyl-2-((4-(3,4-dimethoxyphenyl)-3-oxo-3,4-dihydropyrazin-2-yl)thio)acetamide
3-{[(2-Chloro-6-fluorophenyl)methyl]sulfanyl}-1-(3,4-dimethoxyphenyl)-1,2-dihydropyrazin-2-one