Mefloquine, a clinically useful quinolinemethanol antimalarial which does not significantly bind to DNA

WE report that mefloquine (2,8-bis-(trifluoromethyl)-α-(2-pipe-ridyl)-4-quinolinemethanol1, see Fig. 1) clinically useful against drug-resistant Plasmodium falciparum malaria (G. M. Trenholme, unpublished), does not significantly bind to calf thymus DNA. This constitutes the first reported case of an active compound in the quinoline–acridine class of antimalarials which does not strongly bind to DNA by intercalation.