Diverse dehydroxy-isotebuquine derivatives were prepared by using a five step synthetic sequence in good yields. All these new 4-aminoquinolines were evaluated as inhibitors of haemozoin formation, where most of them showed a significant inhibition value (% IHF >97). The best inhibitors were tested in vivo as potential antimalarials in mice infected with Plasmodium berghei ANKA chloroquine susceptible strain, three of them (11b, 11d and 11h) displayed an antimalarial activity comparable to that of chloroquine.
All Keywords
【저자키워드】 malaria, 4-aminoquinoline, Antimalarial activity, Haemozoin formation, Isotebuquine, β-Hematin,
【저자키워드】 malaria, 4-aminoquinoline, Antimalarial activity, Haemozoin formation, Isotebuquine, β-Hematin,