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含三唑和甾体的硫唑嘌呤衍生物:合成、抗疟和抗利什曼原虫活性。

Thiopurine derivatives containing triazole and steroid: synthesis, antimalarial and antileishmanial activities.

机构信息

Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Campus Universitário, Juiz de Fora, Minas Gerais 36036-900, Brazil.

出版信息

Biomed Pharmacother. 2011 Jun;65(3):198-203. doi: 10.1016/j.biopha.2010.10.013. Epub 2010 Nov 5.

DOI:10.1016/j.biopha.2010.10.013
PMID:21111565
Abstract

A series of novel 6-thiopurine derivates containing 1,2,3-triazole were synthesized and their in vivo antimalarial activity and in vitro antileishmanial activity were examined. The compounds 10, 11, 12 and 14 presented higher values of inhibition of parasite multiplication than chloroquine. For antileishmanial activity, the compound 14 showed activity against the three species of Leishmania tested. None of compounds showed cytotoxicity against mammalian cells.

摘要

合成了一系列新型的含 1,2,3-三唑的 6-硫代嘌呤衍生物,并对它们的体内抗疟活性和体外抗利什曼原虫活性进行了研究。化合物 10、11、12 和 14 对寄生虫增殖的抑制作用高于氯喹。在抗利什曼原虫活性方面,化合物 14 对三种测试的利什曼原虫均有活性。没有一种化合物对哺乳动物细胞表现出细胞毒性。

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