The difficulty of developing an efficient malaria vaccine along with increasing spread of multidrug resistant strain of to the available antimalarial drugs poses the need to discover safe and efficacious antimalarial drugs to control...
moreThe difficulty of developing an efficient malaria vaccine along with increasing spread of multidrug resistant strain of to the available antimalarial drugs poses the need to discover safe and efficacious antimalarial drugs to control malaria. An alternative strategy is to synthesize compounds possessing structures similar to the active natural products or marketed drugs. Several biologically active natural products and drugs contain β-carboline moiety. In the present study, few selected β-carboline derivatives have been synthesized and tested for their in vitro and in vivo antiplasmodial activity against the rodent malaria parasite (NK-65). The designed analogs exhibited considerable in vitro antimalarial activity. Two compounds (1,3)-methyl 1-(benzo[][1,3]dioxol-5-yl)-2,3,4,9-tetrahydro-1-pyrido[3,4-]indole-3-carboxylate () and (1,3)-methyl 1-(pyridin-3-yl)-2,3,4,9-tetrahydro-1-pyrido[3,4-]indole-3-carboxylate () were further selected for in vivo studies. Both the lead compounds ( ...