AI Article Synopsis
- Growing scientific interest in orthopoxvirus infections spurred by the 2022 mpox outbreak has led to a focus on developing new antiviral compounds.
- This research focuses on synthesizing new 2-arylimidazoles that show effectiveness against several orthopoxviruses, including the variola virus.
- Among the various imidazole derivatives, 1-hydroxyimidazoles stand out for their strong antiviral activity and unique structural features, with the most promising compound showing high selectivity against vaccinia and variola viruses.
Article Abstract
Scientific interest in orthopoxvirus infections and search for new highly effective compounds possessing antiviral activity against orthopoxviruses have significantly increased as a result of worldwide mpox outbreak in 2022. The present work deals with the synthesis of new 2-arylimidazoles exhibiting activity not only against the vaccinia virus, cowpox virus and ectromelia (mousepox) virus but also against the variola virus. Among the imidazole derivatives under consideration (1-hydroxyimidazoles, 1-methoxyimidazoles, 1-benzyloxyimidazoles, and imidazole -oxides), the most promising antiviral activity is demonstrated by 1-hydroxyimidazoles, which may exist as two prototropic tautomers. Both of these tautomers may be manifested in different crystal structures of these compounds, according to single-crystal X-ray diffraction analysis, while predominantly one of them (-hydroxy-tautomeric form) is present in DMSO- solutions and in the gaseous state, as shown by NMR spectroscopy and quantum-chemical calculations. The leader compound 1-hydroxy-2-(4-nitrophenyl)imidazole 4a demonstrated the highest selectivity indices against the vaccinia virus (SI = 1072) and the variola virus (SI = 373).
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11331333 | PMC |
| http://dx.doi.org/10.1039/d4md00181h | DOI Listing |
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