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首页> 外文期刊>Parasitology >Simple dialkyl pyrazole-3,5-dicarboxylates show in vitro and in vivo activity against disease-causing trypanosomatids
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Simple dialkyl pyrazole-3,5-dicarboxylates show in vitro and in vivo activity against disease-causing trypanosomatids

机译：简单的二烷基吡唑-3,5-二羧酸盐在体外和体内活动中展示抗病导致的促蛋白酶体

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摘要

The synthesis and antiprotozoal activity of some simple dialkyl pyrazole-3,5-dicarboxylates (compounds 2-6) and their sodium salts (pyrazolates) (compounds 7-9) against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis are reported. In most cases the studied compounds showed, especially against the clinically significant amastigote forms, in vitro activities higher than those of the reference drugs (benznidazole for T. cruzi and glucantime for Leishmania spp.); furthermore, the low non-specific cytotoxicities against Vero cells and macrophages shown by these compounds led to good selectivity indexes, which are 8-72 times higher for T. cruzi amastigotes and 15-113 times higher for Leishmania spp. amastigotes than those of the respective reference drugs. The high efficiency of diethyl ester 3 and its sodium salt 8 against the mentioned protozoa was confirmed by further in vitro assays on infection rates and by an additional in vivo study in a murine model of acute and chronic Chagas disease. The inhibitory capacity of compounds 3 and 8 on the essential iron superoxide dismutase of the aforementioned parasites may be related to the observed anti-trypanosoma-tid activity. The low acute toxicity of compounds 3 and 8 in mice is also reported in this article.
机译：据报道，一些简单的二烷基吡唑-3,5-二羧酸盐（化合物2-6）的合成和抗丙二醇活性及其对Trypanosoma Cruzi，Leishmania Infantum和Leishmania Braziliensis的它们的钠盐（吡唑酸盐）（化合物7-9）。在大多数情况下，所研究的化合物显示出，特别是对临床显着的神经球形形式，体外活性高于参考药物（苯并咪唑的苯并唑和Leishmania SPP的葡萄糖唑.）;此外，这些化合物所示的抗VERO细胞和巨噬细胞的低非特异性细胞毒性导致了良好的选择性指标，对于克鲁齐，对于克鲁齐，对于LeishMania SPP来说，克鲁齐疟疾的良好选择性指数为8-72倍。 amastigotes比各自参考药物的患者。通过进一步的体外测定对所述原种的二乙酯3及其钠盐8对所述原种的高效率和其在急性和慢性棘耳疾病的小鼠模型中的体内研究中进行了进一步的体外测定。化合物3和8对上述寄生虫的必需铁超氧化物歧化酶的抑制能力可能与观察到的抗锥虫瘤菌活性有关。本文还报道了小鼠中化合物3和8的低急性毒性。

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