Synthetic medicinal chemistry of selected antimalarial natural products

Synthesis and in vitro and in vivo evaluation of antimalarial polyamines

“…In the specific case of malaria, the plant natural product quinine (Cinchona sp.) spawned the development of chloroquine, primaquine and mefloquine [2] while investigation of the active principals of the Chinese plant (Artemisia annua) led ultimately to the introduction of artemisinin and related semisynthetic antimalarials [2,3]. While chloroquine and artemisinintype endoperoxides continue to be used in the front-line treatment of malaria, the increased incidence of resistance [4] prompts the need to develop new mode-of-action antimalarials.…”

Use and importance of quina (Cinchona spp.) and ipeca (Carapichea ipecacuanha (Brot.) L. Andersson): Plants for medicinal use from the 16th century to the present

“…Woodward and W.E. Doering, followed by others (Kumar et al, 2009). However, quinine synthesis was not able to compete economically with the isolation of alkaloids from natural or synthetic resources (Cuyubamba et al, 2009;Kumar et al, 2009), although quinine was considered expensive.…”

Plants as antimalarial agents in Sub-Saharan Africa

“…Plant products continue to make an immense contribution to malaria chemotherapy, either directly as antimalarial agents, or as important lead compounds for the discovery of more potent antimalarial drugs (Kumar et al, 2009). Plant agents provide templates for the development of structurally simpler analogues that serve as effective antimalarials.…”