Amuchástegui P I, Moretti E R, Basso B, Sperandeo N, de Bertorello M M
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Argentina.
Rev Argent Microbiol. 1990 Oct-Dec;22(4):199-207.
Knowing the need for new drugs against the etiologic agent of Chagas disease and considering the biological properties of naphthoquinones and isoxazoles, the effect of three isoxazolyl-naphthoquinones on the growth of Trypanosoma cruzi was studied. To evaluate the activity of the compounds on epimastigote forms, growth curves with different concentrations of 2-hydroxi-N-(3,4-dimethyl-5-isoxazolyl)-1,4-naphthoquinone-4 -imine (I), N-(3,4-dimethyl-5-isoxazolyl)-4-amino-1,2-naphthoquinone (II), 2-acetyl-N-(3,4-dimethyl-5-isoxazolyl)-1,4-naphthoquinone-imine (III) and Nifurtimox as reference drug were made. The studies on the trypomastigote form were performed on two month old BALB/c mice, evaluating parasitemia on day 13 post infection. The results obtained with epimastigotes showed that all drugs induced alterations in motility, morphology, viability and/or lysis of parasites. For the treatments on trypomastigotes the best results were obtained with (I) which reduced parasitemia compared to untreated controls.
鉴于对抗查加斯病病原体的新药的需求,并考虑到萘醌和异恶唑的生物学特性,研究了三种异恶唑基萘醌对克氏锥虫生长的影响。为评估化合物对前鞭毛体形式的活性,绘制了不同浓度的2-羟基-N-(3,4-二甲基-5-异恶唑基)-1,4-萘醌-4-亚胺(I)、N-(3,4-二甲基-5-异恶唑基)-4-氨基-1,2-萘醌(II)、2-乙酰基-N-(3,4-二甲基-5-异恶唑基)-1,4-萘醌-亚胺(III)以及作为参比药物的硝呋替莫的生长曲线。对锥鞭毛体形式的研究在两月龄的BALB/c小鼠上进行,评估感染后第13天的寄生虫血症。前鞭毛体的实验结果表明,所有药物均引起寄生虫的运动性、形态、活力和/或裂解的改变。对于锥鞭毛体的治疗,(I)取得了最佳结果,与未治疗的对照组相比,其降低了寄生虫血症。