Antitrypanosomal and antioxidant properties of 4-hydroxycoumarins derivatives

被引:48
作者
Perez-Cruz, Fernanda [2 ]
Serra, Silvia [1 ,3 ]
Delogu, Giovanna [3 ]
Lapier, Michel [2 ]
Diego Maya, Juan [4 ]
Olea-Azar, Claudio [2 ]
Santana, Lourdes [1 ]
Uriarte, Eugenio [1 ]
机构
[1] Univ Santiago de Compostela, Dept Quim Organ, Fac Farm, Santiago De Compostela 15782, Spain
[2] Univ Chile, Dept Quim Inorgan & Analit, Lab Rad Libres & Antioxidantes, Fac Ciencias Quim & Farmaceut, Santiago 1, Chile
[3] Univ Cagliari, Dipartimento Sci Vita & Ambiente, I-09124 Cagliari, Italy
[4] Univ Chile, Fac Med, Dept Farmacol Mol & Clin, Santiago 7, Chile
关键词
4-Hydroxycoumarins; Trypanosoma cruzi; Chagas disease; Antioxidant properties; CHAGAS-DISEASE; TRYPANOSOMA-CRUZI; IN-VITRO; INHIBITORS; COUMARINS; MAO; 3-ARYLCOUMARINS; POTENT;
D O I
10.1016/j.bmcl.2012.07.013
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In the present communication we prepared a series of six 4-hydroxycoumarin derivatives, isosters of quercetin, recognized as an antioxidant natural compound, with the aim of evaluating the antitrypanosomal activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, and the antioxidant properties. We have used the 4-hydroxycoumarin moiety (compound 1) as the molecular template for the synthesis of compounds 2-7. These derivates have shown moderate trypanocidal activity. However they have been proved to be good antioxidants. In particular compound 7 is the most active antioxidant and it is, therefore, a potential candidate for a successful employment in conditions characterized by free radicals overproduction. (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5569 / 5573
页数:5
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