Research Area: Infection Biological Activity: Sulfadoxine(Sulphadoxine) is an ultra-long-lasting sulfonamide with an IC50 of 249 µg/ml for P. vivax. It is often used in combination with pyrimethamine to treat or prevent malaria. Both drugs are antifolates; they inhibit the production of enzymes involved in the synthesis of folic acid within the parasites. Either drug by itself is only moderately effective in treating malaria, because the parasite Plasmodium falciparum may be able to use exogenous folic acid, i.e. folic acid which is present in the parasite’s environment, while in combination, the two substances have a synergistic effect which outbalances that ability. [1][2]
A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections. [PubChem]
Indication
Sulfadoxine is used in combination with pyrimethamine for the treatment or prevention of malaria. It can also be used to treat various infections in livestock as well. Sulfadoxine and pyrimethamine is indicated for the treatment of Plasmodium falciparum malaria in those patients in whom chloroquine resistance is suspected.
Pharmacology
Sulfadoxine helps inhibit the enzyme dihydropteroate synthetase which is an enzyme necessary in the conversion of PABA to folic acid. As folic acid is vital to the synthesis, repair, and methylation of DNA which is vital to cell growth in Plasmodium falciparum. With this vital nutrient lacking, the parasite has difficulty in reproducing.
Application Sulfadoxine is a sulfonamide antibiotic used in combination with pyrimethamine for the treatment or prevention of malaria. It is also used to treat various infections in livestock. Sulfadoxine and pyrimethamine is indicated for the treatment of Plasmodium falciparum malaria in patients where chloroquine resistance is suspected1. It is used to study infections caused by Toxoplasma gondii2 and has been used to prevent infections after surgery during animal studies3. Biochem/physiol Actions Sulfadoxine is a sulfonamide antibacterial that inhibits dihydropteroate synthase (DHPS), an enzyme that transforms 4-aminobenzoic acid (PABA) in the synthesis of dihydropteroic acid. This enzyme is also a component of the folate metabolic pathway and is upstream of dihydrofolate reductase (DHFR).
A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.
参考文献
PubChem文献
数据源提供
• http://en.wikipedia.org/wiki/Sulfadoxine
• Kapoor, V.K., et al.: Anal. Profiles Drug Subs., 17, 571 (1988)