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Easily synthesized antimalarial ferrocene triazacyclononane quinoline conjugates |
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| Authors: | Christophe Biot Jean Dessolin Isabelle Ricard |
| Affiliation: | a UMR 8525 CNRS, Institut de Biologie et Institut Pasteur de Lille, Université de Lille II, 1 rue du Professeur Calmette, BP 447, 59021 Lille, France b Bioinformatique Génomique et Structurale, Université Libre de Bruxelles, CP 165/61, 50 Avenue F.D. Roosevelt, B-1050 Bruxelles, Belgium c UMR CNRS 5144, Institut Européen de Chimie et Biologie, 2 rue Robert Escarpit, 33607 Pessac Cedex, France d INSERM U. 547, Institut Pasteur, 1 rue du Professeur Calmette, BP 245, 59019 Lille, France |
| Abstract: | Starting from triazacyclononane, easily accessible ferrocenic quinoline derivatives were synthesized. Their antiplasmodial properties were investigated against chloroquine sensitive (HB3) and chloroquine-resistant (Dd2) Plasmodium falciparum. One of them, 7-chloro-4-[4-(7-chloro-4-quinolyl)-7-ferrocenylmethyl-1,4,7- triazacyclononan-1-yl]quinoline (4) showed potent antimalarial activity in vitro against the chloroquine-resistant strain Dd2 and therefore revealed to be the most promising lead from the present work for new organometallic antimalarial agents. |
| Keywords: | TACN 1,4,7-triazacyclononane TEA, triethylamine |
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