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. 2023 Jun 9;15(6):1342.
doi: 10.3390/v15061342.

Anticoronavirus Evaluation of Antimicrobial Diterpenoids: Application of New Ferruginol Analogues

Affiliations

Anticoronavirus Evaluation of Antimicrobial Diterpenoids: Application of New Ferruginol Analogues

Mihayl Varbanov et al. Viruses. .

Abstract

The abietane diterpene (+)-ferruginol (1), like other natural and semisynthetic abietanes, is distinguished for its interesting pharmacological properties such as antimicrobial activity, including antiviral. In this study, selected C18-functionalized semisynthetic abietanes prepared from the commercially available (+)-dehydroabietylamine or methyl dehydroabietate were tested in vitro against human coronavirus 229E (HCoV-229E). As a result, a new ferruginol analogue caused a relevant reduction in virus titer as well as the inhibition of a cytopathic effect. A toxicity prediction based on in silico analysis was also performed as well as an estimation of bioavailability. This work demonstrates the antimicrobial and specifically antiviral activity of two tested compounds, making these molecules interesting for the development of new antivirals.

Keywords: abietane; antimicrobial; coronavirus; dehydroabietylamine; phenol; phthalimide.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Natural and semisynthetic antiviral abietanes 17.
Scheme 1
Scheme 1
Synthetic sequence for the preparation of tested molecules 1, 3, and 1216.
Figure 2
Figure 2
Cell viability after 72 h incubation with the compounds at 3.6–82.7 µM (n = 3).
Figure 3
Figure 3
Effect of the compounds on the viral titer of HCoV 229E (n = 1).
Figure 4
Figure 4
Antiviral effect based on the variation of the cell monolayer density and on the HCoV 229E-induced CPE (n = 3).

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