Franks noted that the aminoquinoline
antimalarials represent first-line oral therapy.
Studies of complex formation between the bromophenol blue and some important aminoquinoline
Mutations within the Plasmodium falciparum multidrug-resistant (Pfmdr)1 gene principally the N86Y, Y184F, S1034C, N1042D, and D1246Y were shown to play a modulatory role in further decreasing sensitivity to chloroquine as well as other aminoquinolines
such as amodiaquine (AQ) and mefloquine [13, 14].
It took 15 years to observe a loss of efficacy with aminoquinolines
. Quinine, isolated from Cinchona, is still useful despite more than 350 years of continuous use.
Antimalarial drug resistance has spread and intensified over the last 15-20 years, leading to a dramatic decline in the efficacy of most antimalarial drugs including aminoquinolines
, halofantrine, sulfadoxine-pyrimehtamine etc [6,10,76,50,55].
Structure-function relationships in aminoquinolines
: effect of amino and chloro groups on quinoline-hematin complex formation, Inhibition of -hematin formation, and antiplasmodial activity.