1. In vitro and in vivo antimalarial activity of derivatives of 1,10-phenanthroline framework.
- Author
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Yapi AD, Valentin A, Chezal JM, Chavignon O, Chaillot B, Gerhardt R, Teulade JC, and Blache Y
- Subjects
- Animals, Antimalarials chemical synthesis, Female, HeLa Cells, Humans, In Vitro Techniques, Inhibitory Concentration 50, Malaria prevention & control, Mice, Parasitemia prevention & control, Parasitic Sensitivity Tests, Phenanthrolines chemical synthesis, Plasmodium falciparum classification, Plasmodium falciparum growth & development, Structure-Activity Relationship, Antimalarials pharmacology, Phenanthrolines pharmacology, Plasmodium falciparum drug effects
- Abstract
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 mice infected by P. vinckei petteri showing an ED50 of 7.86 mg/kg/day.
- Published
- 2006
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