新合成的[1,2,4]三唑[1,5a]嘧啶衍生物体外抗克氏锥虫、多诺瓦利什曼原虫和stahelphytomonas的研究

F Luque , C Fernández-Ramos , E Entrala , M.J Rosales , J.A Navarro , M.A Romero , J.M Salas , M Sánchez-Moreno
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引用次数: 16

摘要

新合成的化合物[1,2,4]三唑[1,5a]嘧啶衍生物对克氏锥虫、多诺瓦利什曼原虫和stahelphytomonas的抗原虫活性进行了测试。其中6种化合物显著抑制克氏T. (T. cruzi)、多诺瓦氏L. (L. donovani)和staheli. (P. staheli)的增粗体型体外细胞生长。部分化合物在1 μg/ml浓度下达到完全生长抑制作用48 h。化合物对白纹伊蚊细胞、小鼠巨噬细胞J-774A均无明显毒性。1和esculentum的剂量比用于寄生虫的剂量大5倍。
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In vitro evaluation of newly synthesised [1,2,4]triazolo[1,5a]pyrimidine derivatives against Trypanosoma cruzi, Leishmania donovani and Phytomonas staheli

The antiprotozoal activity of newly synthesised compounds, all [1,2,4]triazolo [1,5a]pyrimidine derivatives, was tested against the protozoan parasites Trypanosoma cruzi, Leishmania donovani and Phytomonas staheli. Six of these compounds significantly inhibited in vitro cell growth of the epimastigote forms of T. cruzi, and the promastigote forms of L. donovani and P. staheli. Some of the compounds reached complete growth inhibition at 1 μg/ml for 48 h of parasite/drug interaction. None of the compounds tested showed significant toxicity against cells of Aedes albopictus, mouse macrophages J-774A.1 and Lycopersicum esculentum at dosages five times greater than used against parasites.

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