期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 126, 期 -, 页码 1129-1135出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.12.017
关键词
Chalcones; Trypanosoma brucei; Trypanosome cruzi; Leishmania infantum; Early toxicity studies; Cyclodextrins formulation
资金
- European Union [603240]
- Ministry of Education and Research (MIUR) [2012-74BNKN]
- COST ACTION [1307]
Chalcones display a broad spectrum of pharmacological activities. Herein, a series of 2'-hydroxy methoxylated chalcones was synthesized and evaluated towards Trypanosoma brucei, Trypanosoma cruzi and Leishmania infantum. Among the synthesized library, compounds 1, 3, 4, 7 and 8 were the most potent and selective anti-T. brucei compounds (EC50 = 13-4.2 mu M, selectivity index >10-fold). Compound 4 showed the best early-tox and antiparasitic profile. The pharmacokinetic studies of compound 4 in BALB/c mice using hydroxypropil-beta-cyclodextrins formulation showed a 7.5 times increase in oral bioavailability. (C) 2016 Elsevier Masson SAS. All rights reserved.
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