无鞭毛体
杜氏利什曼原虫
克鲁兹锥虫
苯硝唑
米尔替芬
利什曼原虫
杀虫药
恰加斯病
IC50型
无菌的
生物
细胞毒性
杀锥虫剂
利什曼病
生物化学
化学
药理学
体外
内脏利什曼病
布氏锥虫
病毒学
免疫学
细菌
寄生虫寄主
计算机科学
万维网
基因
遗传学
作者
Minni Pirttimaa,Abedelmajeed Nasereddin,Dmitry Kopelyanskiy,Marcel Kaiser,Jari Yli‐Kauhaluoma,Kirsi-Marja Oksman-Caldentey,Reto Brun,Charles L. Jaffe,Vânia M. Moreira,Sami Alakurtti
标识
DOI:10.1021/acs.jnatprod.5b00990
摘要
Dehydroabietylamine (1) was used as a starting material to synthesize a small library of dehydroabietyl amides by simple and facile methods, and their activities against two disease-causing trypanosomatids, namely, Leishmania donovani and Trypanosoma cruzi, were assayed. The most potent compound, 10, an amide of dehydroabietylamine and acrylic acid, was found to be highly potent against these parasites, displaying an IC50 value of 0.37 μM against L. donovani axenic amastigotes and an outstanding selectivity index of 63. Moreover, compound 10 fully inhibited the growth of intracellular amastigotes in Leishmania donovani-infected human macrophages with a low IC50 value of 0.06 μM. This compound was also highly effective against T. cruzi amastigotes residing in L6 cells with an IC50 value of 0.6 μM and high selectivity index of 58, being 3.5 times more potent than the reference compound benznidazole. The potent activity of this compound and its relatively low cytotoxicity make it attractive for further development in pursuit of better drugs for patients suffering from leishmaniasis and Chagas disease.
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