Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid
Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid
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DOI：
10.3390/molecules16021166
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发表时间：
2011-02-01
期刊：
影响因子：
4.6
通讯作者：
da Silva, Cleuza C.
中科院分区：
文献类型：
--
作者：
Haraguchi, Shirani K.;Silva, Adriano A.;da Silva, Cleuza C.
以天然二萜香豆烯酸为原料合成了一系列新的硫代氨基脲类化合物，并对克氏锥虫的拟马马体表体进行了抗锥虫活性测试。其中，邻硝基苯甲醛-硫代氨基脲酮衍生物的IC50值为2.0 μ m，是活性最高的化合物。结果表明，所完成的结构修饰增强了这些化合物的抗锥虫活性。此外，硫氰酸酯、硫代氨基脲及其对甲基、对甲氧基、对二甲胺、间硝基和邻氯苯醛代氨基硫代氨基脲衍生物对LLMCK2细胞的毒性较低，IC50为59.5 μ M。
A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC50 values between 2-24.0 mu M. The o-nitrobenzaldehyde- thiosemicarbazone derivative was the most active compound with IC50 of 2.0 mu M. The results show that the structural modifications accomplished enhanced the antitrypanosomal activity of these compounds. Besides, the thiocyanate, thiosemicarbazide and the p- methyl, p-methoxy, p-dimethylamine, m-nitro and o-chlorobenzaldehydethiosemicarbazone derivatives displayed lower toxicity for LLMCK2 cells than kaurenoic acid, exhibing an IC50 of 59.5 mu M.