5c7a7a8bbd6ce0b21f76b2ad90023229 pmc_29337878.pdf d3723d5e93b4c73445b6ccffe7f8bc9b19d51c14 pmc_29337878.pdf 44992fe9c7d94fb4e050b8e05aa60975cc15dbda0f98a61b7a02cb2ffd580ae4 pmc_29337878.pdf Title: Tetrasubstituted Imidazolium Salts as Potent Antiparasitic Agents against African and American Trypanosomiases Subject: Imidazolium salts are privileged compounds in organic chemistry, and have valuable biological properties. Recent studies show that symmetric imidazolium salts with bulky moieties can display antiparasitic activity against T. cruzi. After developing a facile methodology for the synthesis of tetrasubstituted imidazolium salts from propargylamines and isocyanides, we screened a small library of these adducts against the causative agents of African and American trypanosomiases. These compounds display nanomolar activity against T. brucei and low (or sub) micromolar activity against T. cruzi, with excellent selectivity indexes and favorable molecular properties, thereby emerging as promising hits for the treatment of Chagas disease and sleeping sickness. Keywords: imidazolium salts; isocyanides; antiparasitic agents; Trypanosoma brucei; Trypanosoma cruzi Author: Ouldouz Ghashghaei, Nicola Kielland, Marc Revés, Martin C. Taylor, John M. 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