Imidazo[2,1-b]thiazole carbohydrate derivatives: Synthesis and antiviral activity against Junin virus, agent of Argentine hemorrhagic fever
作者:José Sebastián Barradas、María Inés Errea、Norma B. D'Accorso、Claudia Soledad Sepúlveda、Elsa Beatriz Damonte
DOI:10.1016/j.ejmech.2010.11.012
日期:2011.1
imidazo[2,1-b]thiazole. The cyclization step was performed in two different conditions by using either thermal or microwave heating. Comparing the results of both methodologies, we found that the microwave assistance is an improved alternative to obtain this family of heterocyclic compound. Compounds were first evaluated for cytotoxicity in Vero cells by MTT method and then, the antiviral activity was
在这里,我们描述了3,5-二取代的咪唑并[2,1- b ]噻唑的合成。通过使用热或微波加热,在两个不同的条件下进行环化步骤。比较这两种方法的结果,我们发现微波辅助是获得该杂环化合物族的一种改进的替代方法。首先通过MTT方法评估化合物在Vero细胞中的细胞毒性,然后使用JUNV株IV4454作为模型系统,通过在低于相应CC 50的浓度范围内通过病毒产量抑制试验来测定抗病毒活性。活性最高的化合物(3和4)在猴Vero细胞中显示出对JUNV的抗病毒活性水平高于参考物质利巴韦林。然后,它们是有望用于进一步分析和鉴定以建立其对出血热病毒治疗潜力的先导化合物。