EPIROPRIM

Names

[ Name ]:
EPIROPRIM

[Synonym ]:
Ro 11-8958
2,4-Pyrimidinediamine,5-((3,5-diethoxy-4-(1H-pyrrol-1-yl)phenyl)methyl)
Epiroprima [INN-Spanish]
5-((3,5-Diethoxy-4-(1H-pyrrol-1-yl)phenyl)methyl)-2,4-pyrimidinediamine
Epiroprimum [INN-Latin]
Epiroprime [INN-French]
Epiroprim

Biological Activity

[Description]:

Epiroprim (Ro11-8958) is a selective dihydrofolate reductase (DHFR) inhibitor. Epiroprim displays excellent activity against staphylococci, enterococci, pneumococci, and streptococci[1].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

[References]

[1]. H H Locher, et al. Antibacterial activities of epiroprim, a new dihydrofolate reductase inhibitor, alone and in combination with dapsone. Antimicrob Agents Chemother. 1996 Jun;40(6):1376-81.

Chemical & Physical Properties

[ Density]:
1.27g/cm3

[ Boiling Point ]:
626.5ºC at 760 mmHg

[ Molecular Formula ]:
C₁₉H₂₃N₅O₂

[ Molecular Weight ]:
353.41800

[ Flash Point ]:
332.7ºC

[ Exact Mass ]:
353.18500

[ PSA ]:
101.21000

[ LogP ]:
3.98230

[ Index of Refraction ]:
1.629

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV8140650

CHEMICAL NAME :: 2,4-Pyrimidinediamine, 5-((3,5-diethoxy-4-(1H-pyrrol-1-yl)phenyl)methyl)-

CAS REGISTRY NUMBER :: 73090-70-7

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C19-H23-N5-O2

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 :: 1419 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia

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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2 gm/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