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Synthesis of polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth |
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| Authors: | Marion Thévenin Sylviane Thoret Philippe Grellier Joëlle Dubois |
| Institution: | 1. CNRS, Institut de Chimie des Substances Naturelles, UPR2301, Centre de Recherche de Gif, Avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France;2. Muséum National d’Histoire Naturelle, UMR 7245 CNRS, Département RDDM, CP52, 57 rue Cuvier, 75005 Paris, France |
| Abstract: | A series of polysubstituted benzofuran derivatives was easily and rapidly prepared using a tandem Sonogashira coupling/cyclization reaction. Subsequent acylation afforded a small library of 39 new compounds that were assayed in cellulo on Plasmodium falciparum and Trypanosoma brucei parasites. Some of them exhibited good inhibitory activity on T. brucei proliferation. |
| Keywords: | Benzofurans Sonogashira coupling reaction Antiparasitic |
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