Antimalarial drug resistance

Is structural hybridization invoking new dimensions for antimalarial drug discovery research?

“…11,12 Based on the quinine structure, chloroquine (CQ) 13 was developed and used for malarial treatment because of its rapid efficacy and low toxicity. 10 Many other antimalarial drugs belonging to quinolines, such as amodiaquine (AQ), 14 primaquine (PQ), and mefloquine (MQ), 15 were also subsequently developed against chloroquine-resistant (CQR) strains of P. falciparum . 16 Mechanistically, quinolines are recognized to inhibit the polymerization of heme, thus preventing the disposal of polymers from the food vacuole to the cytoplasm where hemozoin is formed and leads to the intra-parasitic accumulation of free heme, which is lethal to the parasite.…”

Non-specific effects of BCG in protozoal infections: tegumentary leishmaniasis and malaria

“…The emergence and spread of antimalarial and antileishmanial drug resistance represent an increasing public health threat. In addition to the oral drug treatment available for leishmaniasis, some patients require several drug injections that are toxic and painful [5,17]. Of note, there is not yet a safe, uniformly effective vaccine available to prevent or treat either disease [18].…”