CIHIDECAR-CONICET - Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón II - Ciudad Universitaria, 1428 Buenos Aires, Argentina.
Eur J Med Chem. 2011 Jan;46(1):259-64. doi: 10.1016/j.ejmech.2010.11.012. Epub 2010 Nov 27.
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.
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。环化步骤分别采用热或微波加热两种不同条件进行。比较两种方法的结果，我们发现微波辅助是获得此类杂环化合物的改进方法。通过 MTT 法首先评估了化合物在 Vero 细胞中的细胞毒性，然后在低于相应 CC（50）的浓度范围内通过病毒产量抑制试验测定了抗病毒活性，使用 JUNV 株 IV4454 作为模型系统。最活性的化合物（3 和 4）在猴 Vero 细胞中对 JUNV 的抗病毒活性优于参考物质利巴韦林。然后，它们是有前途的先导化合物，可进一步分析和表征，以确定其对出血热病毒的治疗潜力。
