Tetrasubstituted imidazolium salts as potent antiparasitic agents against African and American trypanosomiases

Ouldouz Ghashghaei, Nicola Kielland, Marc Revés, Martin C. Taylor, John M. Kelly, Ornella Di Pietro, Diego Muñoz-Torrero, Belén Pérez, Rodolfo Lavilla

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Abstract

© 2018 by the authors. 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.
Original languageEnglish
Article number177
JournalMolecules
Volume23
Issue number1
DOIs
Publication statusPublished - 1 Jan 2018

Keywords

  • Antiparasitic agents
  • Imidazolium salts
  • Isocyanides
  • Trypanosoma brucei
  • Trypanosoma cruzi

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