Malaria is caused by Plasmodium and is responsible for about 780.000 deaths every year. Research of a new antimalarial chemotherapy has become urgent because of parasite resistance to classical drugs. Mefloquine (Lariam�) is a commercial antimalarial drug whose use may induce adverse side effects, such as insomnia, depression, and suicide. All these effects might be related to the accumulation of (-)-erythro-mefloquine into the brain.            To this purpose, we have realized an efficient asymmetric synthesis route of each enantiomeric mefloquine analogs. The obtained compounds were analyzed by biological tests (in vitro activities, cytotoxicity, research of mechanism of action) and showed encouraging results on different Plasmodium falciparum strains (3D7 and W2). Consequently, other tests like in vivo activities and crossing blood-brain barrier are in progress.

Study of asymmetric quinoline methanols as antimalarial compounds

244th National Meeting (2012)

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