Tetrasubstituted Imidazolium Salts as Potent Antiparasitic Agents against African and American Trypanosomiases.


Ghashghaei, O; Kielland, N; Revés, M; Taylor, MC; Kelly, JM; Di Pietro, O; Muñoz-Torrero, D; Pérez, B; Lavilla, R; (2018) Tetrasubstituted Imidazolium Salts as Potent Antiparasitic Agents against African and American Trypanosomiases. Molecules (Basel, Switzerland), 23 (1). ISSN 1420-3049 DOI: https://doi.org/10.3390/molecules23010177

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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.

Item Type: Article
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Pathogen Molecular Biology
PubMed ID: 29337878
Web of Science ID: 425082500168
URI: http://researchonline.lshtm.ac.uk/id/eprint/4646140

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