Imidazo[2,1-b]thiazole carbohydrate derivatives: Synthesis and antiviral activity against Junin virus, agent of Argentine hemorrhagic fever

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• 作者：José ; Sebastiá ; n Barradas ; Marí ; a Iné ; s Errea ; Norma B. D'Accorso ; Claudia Soledad Sepú ; lveda ; Elsa Beatriz Damonte
• 关键词：Imidazo[2 ; 1-b]thiazole ; Carbohydrates ; Antiviral activity ; Junin virus (JUNV) ; Microwave irradiation
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：January 2011
• 年：2011
• 卷：46
• 期：1
• 页码：259-264
• 全文大小：257 K

文摘

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 CC₅₀, 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.