期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 1, 页码 259-264出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.11.012
关键词
Imidazo[2,1-b]thiazole; Carbohydrates; Antiviral activity; Junin virus (JUNV); Microwave irradiation
资金
- Agencia Nacional de Promocion Cientifica y Tecnologica
- Consejo Nacional de Investigaciones Cientificas y Tecnicas (CONICET)
- Universidad de Buenos Aires (UBA), Argentina
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. (C) 2010 Elsevier Masson SAS. All rights reserved.
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