期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 9, 期 7, 页码 629-634出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00053
关键词
Leishmania infantum; promastigote; amastigote; mice model; aminoquinoline
资金
- Ministry of Science and Technological Development of Serbia [172008]
- Serbian Academy of Sciences and Arts, Executive Programme of Scientific and Technological Cooperation between the Italian Republic and the Republic of Serbia
- Ministero dell'Istruzione, dell'Universita e della Ricerca (PRIN) Project [20154JRJPP_004]
In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50 < 1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 < 1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.
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