杀虫药
齐墩果酸
抗寄生虫的
婴儿利什曼原虫
克鲁兹锥虫
抗寄生虫药
萜烯
二萜
化学
细胞毒性
药理学
抗菌剂
利什曼病
生物化学
传统医学
生物
有机化学
医学
体外
替代医学
免疫学
内脏利什曼病
病理
万维网
寄生虫寄主
计算机科学
作者
Mariano Walter Pertino,Celeste Vega,Miriam Rolón,Cathia Coronel,Antonieta Rojas de Arias,Guillermo Schmeda-Hirschmann
出处
期刊:Molecules
[MDPI AG]
日期:2017-02-28
卷期号:22 (3): 369-369
被引量:23
标识
DOI:10.3390/molecules22030369
摘要
Tropical parasitic diseases such as Chagas disease and leishmaniasis are considered a major public health problem affecting hundreds of millions of people worldwide. As the drugs currently used to treat these diseases have several disadvantages and side effects, there is an urgent need for new drugs with better selectivity and less toxicity. Structural modifications of naturally occurring and synthetic compounds using click chemistry have enabled access to derivatives with promising antiparasitic activity. The antiprotozoal activity of the terpenes dehydroabietic acid, dehydroabietinol, oleanolic acid, and 34 synthetic derivatives were evaluated against epimastigote forms of Trypanosoma cruzi and promastigotes of Leishmaniabraziliensis and Leishmania infantum. The cytotoxicity of the compounds was assessed on NCTC-Clone 929 cells. The activity of the compounds was moderate and the antiparasitic effect was associated with the linker length between the diterpene and the triazole in dehydroabietinol derivatives. For the oleanolic acid derivatives, a free carboxylic acid function led to better antiparasitic activity.
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