Synthesis of novel aminoquinoline derivatives has been accomplished and their
activity against malaria strains has been examined. The compounds showed
moderate in vitro antimalarial activity against two P. falciparum strains,
3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three
amino-quinolines were further examined for antimalarial efficacy in a mouse
model using a modified Thompson test. In this model, mice were infected with
P. berghei-infected red blood cells, and drugs were administered orally.
Anti-malarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice,
however, 2/6 mice of the same group survived through day 31, and one of them
was cured.