期刊
MOLECULES
卷 23, 期 1, 页码 -出版社
MDPI AG
DOI: 10.3390/molecules23010177
关键词
imidazolium salts; isocyanides; antiparasitic agents; Trypanosoma brucei; Trypanosoma cruzi
资金
- DGICYT-Spain [CTQ-2015-67870P, SAF2014-57094-R]
- Generalitat de Catalunya [2014 SGR 52, 137, 1189]
- British Heart Foundation
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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据