Camphor-based symmetric diimines as inhibitors of influenza virus reproduction Научная публикация
Журнал |
Bioorganic and Medicinal Chemistry
ISSN: 0968-0896 , E-ISSN: 1464-3391 |
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Вых. Данные | Год: 2014, Том: 22, Номер: 7, Страницы: 2141-2148 Страниц : DOI: 10.1016/j.bmc.2014.02.038 | ||||||
Ключевые слова | Camphor; Diimine derivatives; Antivirals; Influenza | ||||||
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Реферат:
Influenza is a continuing world-wide public health problem that causes significant morbidity and mortality during seasonal epidemics and sporadic pandemics. The purpose of the study was synthesis and investigation of antiviral activity of camphor-based symmetric diimines and diamines. A set of C2-symmetric nitrogen-containing camphor derivatives have been synthesized. The antiviral activity of these compounds was studied against rimantadine- and amantadine-resistant influenza virus A/California/7/09 (H1N1)pdm09 in MDCK cells. The highest efficacy in virus inhibiting was shown for compounds 2a-e with cage moieties bound by aliphatic linkers. The therapeutic index (selectivity index) for 2b exceeded that for reference compounds amantadine, deitiforin and rimantadine almost 10-fold. As shown by structure-activity analysis, the length of the linker has a dramatic effect on the toxicity of compounds. Compound 2e with -C12H24-linker exhibited the lowest toxicity (CTD50 = 2216 mu M). Derivatives of camphor, therefore, can be considered as prospective antiinfluenza compounds active against influenza viruses resistant to adamantane-based drugs. (C) 2014 Elsevier Ltd. All rights reserved.
Библиографическая ссылка:
Sokolova A.S.
, Yarovaya O.I.
, Korchagina D.V.
, Zarubaev V.V.
, Tretiak T.S.
, Anfimov P.M.
, Kiselev O.I.
, Salakhutdinov N.F.
Camphor-based symmetric diimines as inhibitors of influenza virus reproduction
Bioorganic and Medicinal Chemistry. 2014. V.22. N7. P.2141-2148. DOI: 10.1016/j.bmc.2014.02.038 WOS Scopus РИНЦ
Camphor-based symmetric diimines as inhibitors of influenza virus reproduction
Bioorganic and Medicinal Chemistry. 2014. V.22. N7. P.2141-2148. DOI: 10.1016/j.bmc.2014.02.038 WOS Scopus РИНЦ
Файлы:
Полный текст от издателя
Даты:
Опубликована в печати: | 1 апр. 2014 г. |
Идентификаторы:
Web of science | WOS:000334337800014 |
Scopus | 2-s2.0-84897438413 |
РИНЦ | 21870078 |
OpenAlex | W2007597464 |