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

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

Molecules

Laboratory of Organic Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona Science Park, Baldiri Reixac 10-12, 08028 Barcelona, Spain.

Published: January 2018

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 . 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 and low (or sub) micromolar activity against , with excellent selectivity indexes and favorable molecular properties, thereby emerging as promising hits for the treatment of Chagas disease and sleeping sickness.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017328PMC
http://dx.doi.org/10.3390/molecules23010177DOI Listing

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