Novel purine conjugates with N-heterocycles: synthesis and anti-influenza activity

被引：8

作者：

Krasnov, Victor P. ^{[1
,2
]}

Zarubaev, Vladimir V. ^{[3
]}

Gruzdev, Dmitry A. ^{[1
,2
]}

Vozdvizhenskaya, Olga A. ^{[1
]}

Vakarov, Sergey A. ^{[1
]}

Musiyak, Vera V. ^{[1
]}

Chulakov, Evgeny N. ^{[1
]}

Volobueva, Alexandrina S. ^{[3
]}

Sineguobova, Ekaterina O. ^{[3
]}

Ezhikova, Marina A. ^{[1
]}

Kodess, Mikhail, I ^{[1
,2
]}

Levit, Galina L. ^{[1
]}

Charushin, Valery N. ^{[1
,2
]}

机构：

[1] Russian Acad Sci, Postovsky Inst Organ Synth, Ural Branch, 22-20 Sofyi Kovalevskoi St, Ekaterinburg 620108, Russia

[2] Ural Fed Univ, Inst Chem Engn, 28 Mira St, Ekaterinburg 620062, Russia

[3] St Petersburg Pasteur Res Inst Epidemiol & Microb, 14 Mira St, St Petersburg 197101, Russia

来源：

CHEMISTRY OF HETEROCYCLIC COMPOUNDS | 2021年 / 57卷 / 04期

基金：

俄罗斯科学基金会;

关键词：

omega-amino acids; 6-chloropurine; heterocyclic amines; antiviral activity; influenza A and B viruses; BIOLOGICAL EVALUATION; KINETIC RESOLUTION; INFLUENZA; VIRUS;

D O I：

10.1007/s10593-021-02930-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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 omega-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 anti-influenza 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.

引用

页码：498 / 504

页数：7

共 30 条

[1]

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