Design, Synthesis and Antiviral Evaluation of Novel Conjugates of the 1,7,7‐trimethylbicyclo[2.2.1]heptane Scaffold and Saturated N‐heterocycles via 1,2,3‐triazole Linker Научная публикация
Журнал |
Archiv der Pharmazie
ISSN: 0365-6233 , E-ISSN: 1521-4184 |
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Вых. Данные | Год: 2024, Том: 357, Номер: 3, Номер статьи : e2300549, Страниц : 14 DOI: 10.1002/ardp.202300549 | ||||||||||||||
Ключевые слова | lysosomotropic compounds, monoterpenoids derivatives, virus inhibitors | ||||||||||||||
Авторы |
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Организации |
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Реферат:
A new series of heterocyclic derivatives with a 1,7,7-trimethylbicyclo[2.2.1]heptane fragment was designed, synthesised and biologically evaluated. Synthesis of the target compounds was performed using the Cu(I) catalysed cycloaddition reaction. The key starting substances in the click reaction were an alkyne containing a 1,7,7-trimethylbicyclo[2.2.1]heptane fragment and a series of azides with saturated nitrogen-containing heterocycles. Some of the derivatives were found to exhibit strong antiviral activity against Marburg and Ebola pseudotype viruses. Lysosomal trapping assays revealed the derivatives to possess lysosomotropic properties. The molecular modelling study demonstrated the binding affinity between the compounds investigated and the possible active site to be mainly due to hydrophobic interactions. Thus, combining a natural hydrophobic structural fragment and a lysosome-targetable heterocycle may be an effective strategy for designing antiviral agents.
Библиографическая ссылка:
Sokolova A.S.
, Yarovaya O.I.
, Artyushin O.I.
, Sharova E.V.
, Baev D.S.
, Mordvinova E.D.
, Shcherbakov D.N.
, Shnaider T.A.
, Nikitina T.V.
, Esaulkova I.L.
, Ilyina P.A.
, Zarubaev V.V.
, Brel V.K.
, Tolstikova T.G.
, Salakhutdinov N.F.
Design, Synthesis and Antiviral Evaluation of Novel Conjugates of the 1,7,7‐trimethylbicyclo[2.2.1]heptane Scaffold and Saturated N‐heterocycles via 1,2,3‐triazole Linker
Archiv der Pharmazie. 2024. V.357. N3. e2300549 :1-14. DOI: 10.1002/ardp.202300549 WOS Scopus CAPlus PMID OpenAlex
Design, Synthesis and Antiviral Evaluation of Novel Conjugates of the 1,7,7‐trimethylbicyclo[2.2.1]heptane Scaffold and Saturated N‐heterocycles via 1,2,3‐triazole Linker
Archiv der Pharmazie. 2024. V.357. N3. e2300549 :1-14. DOI: 10.1002/ardp.202300549 WOS Scopus CAPlus PMID OpenAlex
Даты:
Поступила в редакцию: | 29 сент. 2023 г. |
Принята к публикации: | 10 нояб. 2023 г. |
Опубликована online: | 30 нояб. 2023 г. |
Опубликована в печати: | 1 мар. 2024 г. |
Идентификаторы БД:
Web of science: | WOS:001111110200001 |
Scopus: | 2-s2.0-85178221033 |
Chemical Abstracts: | 2023:2521548 |
PMID (PubMed): | 38036303 |
OpenAlex: | W4389208632 |