Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1

Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1 Full article

Journal

European Journal of Medicinal Chemistry
ISSN: 0223-5234 , E-ISSN: 1768-3254

Output data

Year: 2017, Volume: 127, Pages: 661-670 Pages count : 10 DOI: 10.1016/j.ejmech.2016.10.035

Tags

Influenza; Camphor derivatives; Antiviral; Cage compounds

Authors

Sokolova Anastasiya S. ^1,2 , Yarovaya Olga I. ^1,2 , Baev Dmitry S. ¹ , Shernyukov Andrey V. ¹ , Shtro Anna A. ³ , Zarubaev Vladimir V. ³ , Salakhutdinov Nariman F. ^1,2

Affiliations

1	(Данные Web of science) Russian Acad Sci, NN Vorozhtsov Novosibirsk Inst Organ Chem, Siberian Branch, Lavrentjev Ave 9, Novosibirsk 630090, Russia
2	(Данные Web of science) Novosibirsk State Univ, Pirogova St 2, Novosibirsk 630090, Russia
3	(Данные Web of science) Influenza Res Inst, Dept Chemotherapy, 15-17 Prof Popova St, St Petersburg 197376, Russia

A series of camphor derived imines was synthesised and evaluated in vitro for antiviral activity. Theoretical evaluations of ADME properties were also carried out. Most of these compounds exhibited significant activity against the drug-resistant strains of influenza A virus. Especially, compounds 2 (SI = 632) and 3 (SI = 417) presented high inhibition against influenza subtypes A/Puerto Rico/8/34 and A/California/07/09 of H1N1pdm09. Analysis of the structure-activity relationship showed that the activity was strongly dependent on the length of the aliphatic chain: derivatives with a shorter chain possessed higher activity, while the suppressing action of compounds with long aliphatic chains was lower. (C) 2016 Elsevier Masson SAS.

Sokolova A.S. , Yarovaya O.I. , Baev D.S. , Shernyukov A.V. , Shtro A.A. , Zarubaev V.V. , Salakhutdinov N.F.
Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1
European Journal of Medicinal Chemistry. 2017. V.127. P.661-670. DOI: 10.1016/j.ejmech.2016.10.035 WOS Scopus РИНЦ

Published print:

Feb 1, 2017

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