Antiviral profiling of c-18- or c-19-functionalized semisynthetic abietane diterpenoids

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 simplextype 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 μM against Colombian Zika virus strains and EC50 = 9.8 μM against Chikungunya virus. Knowing that this ferruginol analogue is also active against Dengue virus type 2 (EC50 = 1.4 μM, DENV-2), we can conclude that this compound is a promising broad-spectrum antiviral agent paving the way for the development of novel antivirals.

• Autores: González Cardenete, Miguel A.; Hamulić, Damir; Miquel Leal, Francisco J.; González Zapata, Natalia; Jiménez Jarava, Orlando J.; Brand, Yaneth M.; Restrepo Méndez, Laura C.; Martínez Gutiérrez, Marlén; Betancur Galvis, Liliana A.; Marín, Maria L.
• Tipo de recurso: Article of investigation
• Fecha de publicación: 2022
• Institución: Universidad Cooperativa de Colombia
• Repositorio: Repositorio UCC
• OAI Identifier: oai:repository.ucc.edu.co:20.500.12494/52298
• Acceso en línea: https://hdl.handle.net/20.500.12494/52298
• Palabra clave: Assays,; Antimicrobial agents; Infectious diseases; Inhibition; Pharmaceuticals
• Rights: openAccess
• License: http://purl.org/coar/access_right/c_abf2