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新合成的[1,2,4]三唑并[1,5-a]嘧啶衍生物对克氏锥虫、杜氏利什曼原虫和斯塔赫利植滴虫的体外评价

In vitro evaluation of newly synthesised [1,2,4]triazolo[1,5a]pyrimidine derivatives against Trypanosoma cruzi, Leishmania donovani and Phytomonas staheli.

作者信息

Luque F, Fernández-Ramos C, Entrala E, Rosales M J, Navarro J A, Romero M A, Salas J M, Sánchez-Moreno M

机构信息

Instituto de Biotecnología, Grupo de Bioquímica y Parasitología Molecular ,Facultad de Ciencias, Universidad de Granada, Spain.

出版信息

Comp Biochem Physiol C Toxicol Pharmacol. 2000 May;126(1):39-44. doi: 10.1016/s0742-8413(00)00093-1.

Abstract

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 Phytotmonas 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 microg/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.

摘要

对新合成的所有[1,2,4]三唑并[1,5a]嘧啶衍生物类化合物的抗原生动物活性进行了测试,测试对象为原生动物寄生虫克氏锥虫、杜氏利什曼原虫和斯塔赫利植原体。其中六种化合物显著抑制了克氏锥虫无鞭毛体形式、杜氏利什曼原虫前鞭毛体形式以及斯塔赫利植原体前鞭毛体形式的体外细胞生长。一些化合物在寄生虫/药物相互作用48小时时,浓度为1微克/毫升时达到完全生长抑制。所测试的化合物在剂量比用于寄生虫的剂量大五倍时,均未显示出对白纹伊蚊细胞、小鼠巨噬细胞J-774A.1和番茄有显著毒性。

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