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. 2013 Sep 1;21(17):4885-92.
doi: 10.1016/j.bmc.2013.07.002. Epub 2013 Jul 12.

Synthesis of polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth

Marion Thévenin  1 , Sylviane Thoret, Philippe Grellier, Joëlle Dubois
Affiliations

Synthesis of polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth

Marion Thévenin et al. Bioorg Med Chem. .

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: Antiparasitic; Benzofurans; P. falciparum; Sonogashira coupling reaction; T. brucei.

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