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

✍ Scribed by Ange-Désiré Yapi; Alexis Valentin; Jean-Michel Chezal; Olivier Chavignon; Bernard Chaillot; Roseline Gerhardt; Jean-Claude Teulade; Yves Blache

Publisher: John Wiley and Sons
Year: 2006
Tongue: English
Weight: 643 KB
Volume: 339
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.200500246

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✦ Synopsis

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 mices infected by P. vinckei petteri showing an ED~50~ of 7.86 mg/kg/day.

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