In Vitro and in Vivo Antimalarial Activity of Derivatives of 1,10‐Phenanthroline Framework

A series of trisubstituted 1,10‐phenanthrolines was prepared. These compounds exhibited mild to high biological activities in vitro both toward chloroquino‐resistant FcB1‐Columbia and FcM29‐Cameron strains and Nigerian chloroquino‐sensitive strain of Plasmodium falciparum . Cytotoxicity of the most active compounds was estimated showing that one compound ( 10 ) exhibited a selective activity against malaria parasite (selectivity indexes of 52 and 144). Antiplasmodial activity of this derivative was optimized by N ‐10 alkylation and the phenanthrolinium salt ( 15 ) submitted to an in vivo study using mices infected by P. vinckei petteri showing an ED 50 of 7.86 mg/kg/day.