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三种新型 5-甲基-1,2,4-三唑并[1,5-a]嘧啶-7(4H)-酮基配合物的抗锥虫原生动物的体外和体内活性。

In vitro and in vivo antiparasital activity against Trypanosoma cruzi of three novel 5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7(4H)-one-based complexes.

机构信息

Departamento de Química Inorgánica, Universidad de Granada, Severo Ochoa s/n, Granada, Spain.

出版信息

J Inorg Biochem. 2011 Jun;105(6):770-6. doi: 10.1016/j.jinorgbio.2011.03.015. Epub 2011 Mar 30.

Abstract

Conventional reactions of the versatile multidentate ligand 5-methyl-1,2,4-triazolo[1,5-a] pyrimidin-7(4H)-one (HmtpO) with metallic(II) perchlorate salts lead to three novel multidimensional complexes Cu(HmtpO)(2)(H(2)O)(3)(2)·H(2)O (1), {Cu(HmtpO)(2)(H(2)O)(2)(2) ·2HmtpO}(n) (2) and {Co(HmtpO)(H(2)O)(3)(2)·2H(2)O}(n) (3). We have tested the antiparasital activity in vitro and in vivo of the three new complexes against Trypanosoma cruzi showing very promising results and overcoming clearly the reference drug commonly used for the Chagas disease treatment, benznidazole.

摘要

多功能多齿配体 5-甲基-1,2,4-三唑并[1,5-a]嘧啶-7(4H)-酮(HmtpO)与高氯酸金属(II)盐的常规反应生成了三种新型多维配合物Cu(HmtpO)(2)(H2O)(3)2·H2O (1)、{Cu(HmtpO)(2)(H2O)(2)2·2HmtpO}(n) (2)和{Co(HmtpO)(H2O)(3)2·2H2O}(n) (3)。我们已经测试了这三种新配合物对 Trypanosoma cruzi 的体外和体内抗寄生虫活性,结果非常有前景,明显优于用于治疗恰加斯病的常用药物苯并咪唑。

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