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NOVEL PURINE CONJUGATES WITH N-HETEROCYCLES: SYNTHESIS AND ANTI-INFLUENZA ACTIVITY

Виктор П. Краснов, Владимир В. Зарубаев, Дмитрий А. Груздев, Ольга А. Воздвиженская, Сергей А. Вакаров, Вера В. Мусияк, Евгений Н. Чулаков, Александрина С. Волобуева, Екатерина О. Синегубова, Марина А. Ежикова, Михаил И. Кодесс, Галина Л. Левит, Валерий Н. Чарушин
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Abstract


A number of novel amides were synthesized by coupling of 6-[(9H-purin-6-yl)amino]hexanoic acid to heterocyclic amines. The antiviral activity of the obtained compounds, as well as of purine conjugates in which 7,8-difluoro-3-methyl-3,4-dihydro-2H-1,4-benzoxazine is linked to position 6 of purine through a fragment of ɷ-amino acids with varying lengths of polymethylene chains against influenza A and B viruses was studied in vitro. Purine derivatives have been shown to have moderate activity against influenza A (H1N1) virus. The antiinfluenza activity and cytotoxicity of conjugates with 7,8-difluoro-3-methyl-3,4-dihydro-2H-1,4-benzoxazine depend on the length of the linker fragment.

Keywords


ɷ-amino acids; 6-chloropurine; heterocyclic amines; antiviral activity; influenza A and B viruses.

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