Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi

被引：84
作者：
de Souza, VA
da Silva, R
Pereira, AC
Royo, VD
Saraiva, J
Montanheiro, M
de Souza, GHB
da Silva, AA
Grando, MD
Donate, PM
Bastos, JK
Albuquerque, S
Silva, MLAE
机构：
[1] Univ Franca, BR-14404600 Franca, SP, Brazil
[2] Univ Sao Paulo, Fac Ciencias Farmaceut, BR-14049 Ribeirao Preto, SP, Brazil
[3] Univ Sao Paulo, Fac Filosofia, Dept Quim, BR-14049 Ribeirao Preto, SP, Brazil
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 02期
基金：
巴西圣保罗研究基金会;
关键词：
lignans dibenzylbutyrolactones; trypanocidal activity; amastigote forms; cubebin derivatives;
D O I：
10.1016/j.bmcl.2004.10.079
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Five (-)-cubebin derivative compounds, (-)-O-acetyl cubebin (3), (-)-O-benzyl cubebin (4), (-)-O-(N,N-dimethylaminoethyl)-cubebin (5), (-)-hinokinin (6) and (-)-6,6'-dinitrohinokinin (7), previously synthesised by our research group, were evaluated on in vitro assay against free amastigote forms of Trypanosoina cruzi, the asogic agent of Chagas' disease. It was observed that 6 was the most active compound (IC50 = 0.7 muM), and that 4 and 5 displayed moderate activity against the parasite, giving IC50 values of 5.7 and 4.7 muM, respectively. In contrast, it was observed that compound 3 was inactive and that 7 displayed low activity with IC50 values of congruent to1.5 x 10(4) and 95.3 muM, respectively. (C) 2004 Elsevier Ltd. All rights reserved.
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页码：303 / 307
页数：5
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