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Pyrimethamine

乙胺嘧啶

Mechanism of action:

Pyrimethamine 是一種二氨基嘧啶類(diaminopyrimidine)衍生物。Pyrimethamine 會高親和力結合並抑制原蟲,如弓形蟲(Toxoplasma gondii)、瘧原蟲(Plasmodium spp.)的二氫葉酸還原酶(dihydrofolate reductase),阻斷二氫葉酸(dihydrofolic acid)轉換為四氫葉酸(tetrahydrofolic acid),使 DNA 與 RNA 合成受阻。

​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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