Uses
It is a potent and selective inhibitor of bacterial dihydrofolate reductase, the enzyme responsible for the NADPH-dependent reduction of 7,8-dihydrofolate to 5,6,7,8-tetrahydrofolate. Antibacterial.This compound is a contaminant of emerging concern (CECs).
Definition
ChEBI: 5-[(4,5-dimethoxy-2-methylphenyl)methyl]pyrimidine-2,4-diamine is a dimethoxybenzene.
Synthesis Reference(s)
Journal of Medicinal Chemistry, 14, p. 462, 1971
DOI: 10.1021/jm00287a029
in vivo
Ormetoprim (8.3 mg/kg; i.p.) exhibits absorption half-life (5.4 h), elimination half-life (7.5 h) and Cmax (1.2±0.2 μg/mL)[3].
Ormetoprim (8.3 mg/kg; p.o.) exhibits absorption half-life (3.9 h), elimination half-life (3.9 h), Cmax (1.6±0.4 μg/mL) and oral availability (78.5%) relative to intraperitoneal administration[3].
| Animal Model: | Hybrid striped bass (565-805 g)[3] |
| Dosage: | 50 mg/kg Sulfadimethoxine and Ormetoprim in a 5:1 ratio (Pharmacokinetic Analysis) |
| Administration: | I.p. and p.o. administration |
| Result: | I.p.: t1/2(elim)=7.5 h; t1/2(abs)=5.4 h; Cmax=1.2 μg/mL.
P.o.: t1/2(elim)=3.9 h; t1/2(abs)=3.9 h; Cmax=1.6 μg/mL; F=78.5%.
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