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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Imidazo(2,1-b)thiazole carbohydrate derivatives: Synthesis and antiviral activity against Junin virus, agent of Argentine hemorrhagic fever.
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Imidazo(2,1-b)thiazole carbohydrate derivatives: Synthesis and antiviral activity against Junin virus, agent of Argentine hemorrhagic fever.

机译：咪唑并（2,1-b）噻唑碳水化合物衍生物：对阿根廷出血热病原人胡宁病毒的合成和抗病毒活性。

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摘要

Herein, we describe the syntheses of 3,5-disubstituted 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 assayed by a virus yield inhibition assay in the range of concentrations lower than the corresponding CC(50), using JUNV strain IV4454 as the model system. The most active compounds (3 and 4), showed a level of antiviral activity against JUNV in monkey Vero cells better than the reference substance ribavirin. Then, they are promising lead compound for further analysis and characterization to establish their therapeutic potential against hemorrhagic fever viruses.
机译：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）浓度范围内的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，优于参考物质利巴韦林。然后，它们有望用于进一步的分析和表征，以确立其对出血热病毒的治疗潜力。

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