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Título: | Antiviral Profiling of C18- or C19-Functionalized Semisynthetic Abietane Diterpenoids |
Autor: | González-Cardenete, Miguel A. CSIC ORCID ; Hamulic, Damir; Miquel-Leal, Francisco Javier; González-Zapata, Natalia; Jimenez-Jarava, Orlando J.; Brand, Yaneth M.; Restrepo-Mendez, Laura C.; Martinez-Gutierrez, Marlen; Betancur-Galvis, Liliana A.; Marín, María Luisa CSIC ORCID CVN | Fecha de publicación: | 15-ago-2022 | Editor: | ACS Publications | Citación: | Journal of Natural Products 85(8): 2044-2051 (2022) | Resumen: | Viral infections affect several million patients annually. Although hundreds of viruses are known to be pathogenic, only a few can be treated in the clinic with available antiviral drugs. Naturally based pharmacotherapy may be a proper alternative for treating viral diseases. Several natural and semisynthetic abietane-type diterpenoids have shown important antiviral activities. In this study, a biological evaluation of a number of either C-18- or C-19-functionalized known semisynthetic abietanes against Zika virus, Dengue virus, Herpes virus simplex type 1, and Chikungunya virus are reported. Semisynthetic abietane ferruginol and its analogue 18-(phthalimid-2-yl)ferruginol displayed broad-spectrum antiviral properties. The scale-up synthesis of this analogue has been optimized for further studies and development. This molecule displayed an EC50 between 5.0 and 10.0 ¿M against Colombian Zika virus strains and EC50 = 9.8 ¿M against Chikungunya virus. Knowing that this ferruginol analogue is also active against Dengue virus type 2 (EC50 = 1.4 ¿M, DENV-2), we can conclude that this compound is a promising broad-spectrum antiviral agent paving the way for the development of novel antivirals. | Versión del editor: | http://dx.doi.org/10.1021/acs.jnatprod.2c00464 | URI: | http://hdl.handle.net/10261/287514 | DOI: | 10.1021/acs.jnatprod.2c00464 | Identificadores: | doi: 10.1021/acs.jnatprod.2c00464 issn: 0163-3864 |
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Antiviral_Profiling.pdf | 3,35 MB | Adobe PDF | Visualizar/Abrir |
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