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In Vitro and in Vivo Antimalarial Activity of Derivatives of 1,10‐Phenanthroline Framework
Author(s) -
Yapi AngeDésiré,
Valentin Alexis,
Chezal JeanMichel,
Chavig Olivier,
Chaillot Bernard,
Gerhardt Roseline,
Teulade JeanClaude,
Blache Yves
Publication year - 2006
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200500246
Subject(s) - plasmodium falciparum , in vivo , in vitro , chemistry , phenanthroline , cytotoxicity , derivative (finance) , biological activity , alkylation , stereochemistry , selectivity , malaria , combinatorial chemistry , biochemistry , biology , organic chemistry , immunology , microbiology and biotechnology , economics , financial economics , catalysis
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.
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