الفهرس | Only 14 pages are availabe for public view |
Abstract Antimalarial results revealed that more than 50% of tested compounds possessed over 80% of in vivoantimalarial activity against P. berghei. Among these, compound 39cshowed 100% inhibition. Active compounds were further tested for their in vitro antimalarial activity against chloroquine-resistant strain (RKL9) of P. falciparum and all of them showed an outstanding IC50values in micromolar ranges better than the standard chloroquine phosphate. Compounds 9b, 22b, 35b and 39cshowed comparable activity to pyrimethamine with IC50value equal to 0.0122, 0.0124, 0.0132and 0.0108 μM, respectively. The binding pattern of these active compounds into PfDHFR-TS active site were examined to give insights about their possible mechanism of action. |