posted on 2022-08-15, 20:20authored byMiguel A. González-Cardenete, Damir Hamulić, Francisco J. Miquel-Leal, Natalia González-Zapata, Orlando J. Jimenez-Jarava, Yaneth M. Brand, Laura C. Restrepo-Mendez, Marlen Martinez-Gutierrez, Liliana A. Betancur-Galvis, Maria L. Marín
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.