Next Article in Journal
Functional Impact of the N-terminal Arm of Proline Dehydrogenase from Thermus thermophilus
Previous Article in Journal
Two Novel Proline-Containing Catechin Glucoside from Water-Soluble Extract of Codonopsis pilosula
Previous Article in Special Issue
Multienzyme Biosynthesis of Dihydroartemisinic Acid
Open AccessCommunication

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

1
Laboratory of Organic Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona Science Park, Baldiri Reixac 10-12, 08028 Barcelona, Spain
2
Department of Pathogen Molecular Biology, London School of Hygiene and Tropical Medicine, London WC1E 7HT, UK
3
Laboratory of Pharmaceutical Chemistry (CSIC Associated Unit), Faculty of Pharmacy and Food Sciences, and Institute of Biomedicine (IBUB), University of Barcelona, 08028 Barcelona, Spain
4
Department of Pharmacology, Therapeutics and Toxicology, Institute of Neurosciences, Autonomous University of Barcelona, 08193 Bellaterra, Barcelona, Spain
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(1), 177; https://doi.org/10.3390/molecules23010177
Received: 29 November 2017 / Revised: 10 January 2018 / Accepted: 13 January 2018 / Published: 16 January 2018
(This article belongs to the Special Issue Multicomponent Reaction-Based Synthesis of Bioactive Molecules)
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. View Full-Text
Keywords: imidazolium salts; isocyanides; antiparasitic agents; Trypanosoma brucei; Trypanosoma cruzi imidazolium salts; isocyanides; antiparasitic agents; Trypanosoma brucei; Trypanosoma cruzi
Show Figures

Graphical abstract

MDPI and ACS Style

Ghashghaei, O.; Kielland, N.; Revés, M.; Taylor, M.C.; Kelly, J.M.; Di Pietro, O.; Muñoz-Torrero, D.; Pérez, B.; Lavilla, R. Tetrasubstituted Imidazolium Salts as Potent Antiparasitic Agents against African and American Trypanosomiases. Molecules 2018, 23, 177.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Search more from Scilit
 
Search
Back to TopTop