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Pyrimethamine


Mechanism of action:

Pyrimethamine is a diaminopyrimidine derivative. Pyrimethamine binds with high affinity to and inhibits dihydrofolate reductase in protozoa such as Toxoplasma gondii and Plasmodium spp., blocking the conversion of dihydrofolic acid to tetrahydrofolic acid and thereby impairing DNA and RNA synthesis.

Reference(s):

1. Gatton ML et al. (2004). Evolution of resistance to sulfadoxine-pyrimethamine in Plasmodium falciparum. Antimicrob Agents Chemother. 


2. Sirichaiwat C et al. (2004). Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum. J Med Chem.

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