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- Title
Synthesis and Antiviral Activity of 21β-Acetyl-20β,28-Epoxy-18α,19βH-Ursane Derivatives Against Influenza H1N1 and SARS-Cov-2 Spike Pseudovirus.
- Authors
Khusnutdinova, E. F.; Galimova, Z. I.; Petrova, A. V.; Tretyakova, E. V.; Smirnova, I. E.; Slita, A. V.; Fedij, S. V.; Zarubaev, V. V.; Xiao, S.; Ma, X.; Zhou, D.; Rybalova, T. V.; Polovyanenko, D. N.; Kazakova, O. B.
- Abstract
Allobetulin derivatives with rearranged E-ring exhibit important pharmacological properties against various viral pathogens. Basing on 3β-acetoxy-21β-acetyl-20β,28-epoxy-18α,19βH-ursane triterpenoid, obtained from allobetulin in one stage, a series of new derivatives have been synthesized and their antiviral activity against both influenza virus A (H1N1) and SARS-CoV-2 pseudovirus was evaluated. Among them, 2,3-indolo-allobetulone N-propargyl derivatives were the most efficacious against influenza virus with low toxicity (CC50 × 300 μM) and IC50 values of 7.04 to 3.5 μM and high selectivity indexes (SI 43 and 86). Compared with amodiaquine, a derivative with 3-pyridinylidene fragment 12 showed a weak antiviral activity against SARS-CoV-2 pseudovirus with an inhibition rate of 57.3% at a concentration of 20 μM. Further optimization to increase the cellular antiviral activity seems to be necessary to develop this series of triterpenoids as antiviral agents.
- Subjects
H1N1 influenza; SARS-CoV-2; INFLUENZA viruses; ANTIVIRAL agents; TRITERPENOIDS
- Publication
Chemistry of Natural Compounds, 2024, Vol 60, Issue 2, p275
- ISSN
0009-3130
- Publication type
Article
- DOI
10.1007/s10600-024-04302-w