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- Title
Tetrasubstituted Imidazolium Salts as Potent Antiparasitic Agents against African and American Trypanosomiases.
- Authors
Ghashghaei, Ouldouz; Kielland, Nicola; Revés, Marc; Taylor, Martin C.; Kelly, John M.; Di Pietro, Ornella; Muñoz-Torrero, Diego; Pérez, Belén; Lavilla, Rodolfo
- Abstract
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.
- Subjects
IMIDAZOLES; ANTIPARASITIC agents; TRYPANOSOMIASIS treatment; CHAGAS' disease treatment; TREATMENT of African trypanosomiasis
- Publication
Molecules, 2018, Vol 23, Issue 1, p177
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23010177