The geographic extension of Plasmodium falciparum necessitates the development of new antimalarial drugs that are active against resistant parasite strains. 1 Mefloquine (1) has been shown to have high efficacy for both treatment and prophylaxis of chloroquine-resistant malaria (Fig. 1). 2 However, its present potential is limited due to its adverse central nervous system (CNS) effects, including anxiety, depression, hallucinations, and seizures. 3 One explanation for ...