Tetroxoprim

Names

[ Name ]:
Tetroxoprim

[Synonym ]:
Tetroxoprima
Tetroxoprime [INN-French]
Tetroxoprimum [INN-Latin]
Tetroxoprime
Tetroxoprim
Tetroxoprimum
He 781
Tetroxoprima [INN-Spanish]
Tetroxoprima [Spanish]

Biological Activity

[Description]:

Tetroxoprim is an antimicrobial DHFR inhibitor[1].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate

Research Areas >> Inflammation/Immunology

[In Vitro]

Tetroxoprim brings about a 50% in vitro inhibition with E. coli, at a concentration of 4 x 10-9M[1].

[References]

[1]. H S Aschhoff, et al. Tetroxoprim--a new inhibitor of bacterial dihydrofolate reductase. J Antimicrob Chemother. 1979 Nov;5(B):19-25.

Chemical & Physical Properties

[ Density]:
1.232g/cm3

[ Boiling Point ]:
564.1ºC at 760mmHg

[ Molecular Formula ]:
C₁₆H₂₂N₄O₄

[ Molecular Weight ]:
334.37

[ Flash Point ]:
294.9ºC

[ Exact Mass ]:
334.16400

[ PSA ]:
114.74000

[ LogP ]:
2.43660

[ Index of Refraction ]:
1.587

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV8190000

CHEMICAL NAME :: Pyrimidine, 2,4-diamino-5-(3,5-dimethoxy-4-(2-methoxyethoxy)benzy l)-

CAS REGISTRY NUMBER :: 53808-87-0

BEILSTEIN REFERENCE NO. :: 4271695

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C16-H22-N4-O4

MOLECULAR WEIGHT :: 334.42

WISWESSER LINE NOTATION :: T6N CNJ BZ DZ E1R CO1 EO1 DO2O1

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 :: 1172 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,895,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,895,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1060 mg/kg

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

REFERENCE :: JCHEEU Journal of Chemotherapy. (Edizioni Riviste Scientifiche, via R. Giuliani, 419, 50141 Florence, Italy) V.1- 1989- Volume(issue)/page/year: 5,400,1993

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1410 mg/kg

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

REFERENCE :: JCHEEU Journal of Chemotherapy. (Edizioni Riviste Scientifiche, via R. Giuliani, 419, 50141 Florence, Italy) V.1- 1989- Volume(issue)/page/year: 5,400,1993

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 192 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,895,1979

Safety Information

[ Hazard Codes ]:
Xi

[ 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%