Evaluation of 7-arylaminopyrazolo[1,5-a]pyrimidines as anti-Plasmodium falciparum, antimalarial, and Pf-dihydroorotate dehydrogenase inhibitors
文摘
7-arylpyrazolo[1,5-a]pyrimidines were designed and synthesized as antiplasmodial. Compounds were tested against P. falciparum as antimalarial and as PfDHODH inhibitors. In P. falciparum the IC50 values have been from 1.2 to 88.2 μM. Parasitemia in P. berghei was reduced by 50% on the 5th day inoculation. The docking results agreed with the values obtained from enzymatic assays.