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  • Title: In vitro and in vivo antimalarial activity of derivatives of 1,10-phenanthroline framework.
    Author: Yapi AD, Valentin A, Chezal JM, Chavignon O, Chaillot B, Gerhardt R, Teulade JC, Blache Y.
    Journal: Arch Pharm (Weinheim); 2006 Apr; 339(4):201-6. PubMed ID: 16586427.
    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.
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