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(+)-fenchol and (-)-isopinocampheol derivatives targeting the entry process of filoviruses.
Sokolova, Anastasiya S; Baev, Dmitriy S; Mordvinova, Ekaterina D; Yarovaya, Olga I; Volkova, Natalia V; Shcherbakov, Dmitriy N; Okhina, Alina A; Rogachev, Artem D; Shnaider, Tatiana A; Chvileva, Anastasiya S; Nikitina, Tatiana V; Tolstikova, Tatyana G; Salakhutdinov, Nariman F.
Afiliación
  • Sokolova AS; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences (SB RAS), Novosibirsk, 630090, Russian Federation. Electronic address: asokolova@nioch.nsc.ru.
  • Baev DS; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences (SB RAS), Novosibirsk, 630090, Russian Federation; SRF SKIF, Koltsovo, Novosibirsk Oblast, 630559, Russian Federation.
  • Mordvinova ED; State Research Center of Virology and Biotechnology VECTOR (Rospotrebnadzor), Koltsovo, Novosibirsk Oblast, 630559, Russian Federation.
  • Yarovaya OI; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences (SB RAS), Novosibirsk, 630090, Russian Federation.
  • Volkova NV; State Research Center of Virology and Biotechnology VECTOR (Rospotrebnadzor), Koltsovo, Novosibirsk Oblast, 630559, Russian Federation.
  • Shcherbakov DN; State Research Center of Virology and Biotechnology VECTOR (Rospotrebnadzor), Koltsovo, Novosibirsk Oblast, 630559, Russian Federation.
  • Okhina AA; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences (SB RAS), Novosibirsk, 630090, Russian Federation.
  • Rogachev AD; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences (SB RAS), Novosibirsk, 630090, Russian Federation.
  • Shnaider TA; Institute of Cytology and Genetics (ICG), SB RAS, Novosibirsk, 630090, Russian Federation.
  • Chvileva AS; Novosibirsk State University, Novosibirsk, 630090, Russian Federation.
  • Nikitina TV; Research Institute of Medical Genetics, Tomsk National Research Medical Center, Russian Academy of Sciences, Tomsk, 634050, Russian Federation.
  • Tolstikova TG; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences (SB RAS), Novosibirsk, 630090, Russian Federation.
  • Salakhutdinov NF; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences (SB RAS), Novosibirsk, 630090, Russian Federation.
Eur J Med Chem ; 275: 116596, 2024 Sep 05.
Article en En | MEDLINE | ID: mdl-38889610
ABSTRACT
The increasing frequency of filovirus outbreaks in African countries has led to a pressing need for the development of effective antifilovirus agents. In continuation of our previous research on the antifilovirus activity of monoterpenoid derivatives, we synthesized a series of (+)-fenchol and (-)-isopinocampheol derivatives by varying the type of heterocycle and linker length. Derivatives with an N-alkylpiperazine cycle proved to be the most potent antiviral compounds, with half-maximal inhibitory concentration (IC50) 1.4-20 µÐœ against Lenti-EboV-GP infection and 11.3-47 µÐœ against Lenti-MarV-GP infection. Mechanism-of-action experiments revealed that the compounds may exert their action by binding to surface glycoproteins (GPs). It was demonstrated that the binding of the synthesized compounds to the Marburg virus GP is less efficient as compared to the Ebola virus GP. Furthermore, it was shown that the compounds possess lysosomotropic properties. Thus, the antiviral activity may be due to dual effects. This study offers new antiviral agents that are worthy of further exploration.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales Límite: Animals / Humans Idioma: En Revista: Eur J Med Chem Año: 2024 Tipo del documento: Article Pais de publicación: Francia
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales Límite: Animals / Humans Idioma: En Revista: Eur J Med Chem Año: 2024 Tipo del documento: Article Pais de publicación: Francia