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http://hdl.handle.net/2445/121412
Title: | Tetrasubstituted imidazolium salts as potent antiparasitic agents against African and American trypanosomiases |
Author: | Ghashghaei, Ouldouz Kielland, Nicola Revés, Marc Taylor, Martin C. Kelly, John M. Di Pietro, O. Muñoz-Torrero López-Ibarra, Diego Pérez, Belén Lavilla Grífols, Rodolfo |
Keywords: | Imidazoles Agents antiinfecciosos Tripanosoma Imidazoles Anti-infective agents Trypanosoma |
Issue Date: | 16-Jan-2018 |
Publisher: | MDPI |
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. |
Note: | Reproducció del document publicat a: https://doi.org/10.3390/molecules23010177 |
It is part of: | Molecules, 2018, vol. 23, num. 177 |
URI: | http://hdl.handle.net/2445/121412 |
Related resource: | https://doi.org/10.3390/molecules23010177 |
ISSN: | 1420-3049 |
Appears in Collections: | Articles publicats en revistes (Institut de Biomedicina (IBUB)) Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) |
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