| Autor: |
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. |
| Předmět: |
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| Zdroj: |
Chemistry of Natural Compounds; Mar2024, Vol. 60 Issue 2, p275-282, 8p |
| Abstrakt: |
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. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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