Synthesis of berberine derivatives and their antiviral activity toward respiratory syncytial virus

Synthesis of berberine derivatives and their antiviral activity toward respiratory syncytial virus Full article

Journal

Medicinal Chemistry Research
ISSN: 1054-2523 , E-ISSN: 1554-8120

Output data

Year: 2023, Volume: 32, Number: 11, Pages: 2325-2333 Pages count : 9 DOI: 10.1007/s00044-023-03138-3

Authors

Shtro Anna A. ¹ , Gladkova Elizaveta D. ² , Galochkina Anastasia V. ¹ , Nikolaeva Yulia V. ¹ , Garshinina Angelika V. ¹ , Razgulyaeva Darya N. ¹ , Sorokin Evgeniy V. ¹ , Tsareva Tatyana R. ¹ , Luzina Olga A. ² , Salakhutdinov Nariman F. ²

Affiliations

1	Smorodintsev Research Institute of Influenza (a Russian Ministry of Health federal institution)
2	N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry of Siberian Branch of Russian Academy of Sciences

Funding (1)

Российский Научный Фонд

21-13-00026

A series of derivatives of berberine was synthesized to estimate their antiviral activity toward respiratory syncytial virus. Berberine and its hydrogenated analogs were modified at different positions with various substituents. The antiviral activity of berberine and its derivatives against respiratory syncytial virus strain A2 was studied in vitro. Berberine itself and its 12-nitro and 9-O derivatives having heterocyclic motifs in the substituent were shown to have the highest antiviral activity, with half-maximal inhibitory concentration in the lower range (<10 μM). It was found that half-maximal cytotoxic concentration of the compounds varies widely, from 9 to >2000 μM. The selectivity of most compounds under study was below a desired threshold; only berberine, 12-nitroberberine, and tetrahydroberberine can be considered promising for the development of drugs for respiratory syncytial infection.

Shtro A.A. , Gladkova E.D. , Galochkina A.V. , Nikolaeva Y.V. , Garshinina A.V. , Razgulyaeva D.N. , Sorokin E.V. , Tsareva T.R. , Luzina O.A. , Salakhutdinov N.F.
Synthesis of berberine derivatives and their antiviral activity toward respiratory syncytial virus
Medicinal Chemistry Research. 2023. V.32. N11. P.2325-2333. DOI: 10.1007/s00044-023-03138-3 РИНЦ

Submitted:	Jun 13, 2023
Accepted:	Aug 7, 2023
Published print:	Aug 18, 2023

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