Synthesis and anti-viral activity of azolo-adamantanes against influenza A virus

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• 作者：Vladimir V. Zarubaev ; Efim L. Golod ; Pavel M. Anfimov ; Anna A. Shtro ; Victor V. Saraev ; Alexey S. Gavrilov ; Alex ; er V. Logvinov ; Oleg I.Kiselev
• 关键词：Azoles ; Adamantane derivatives ; Influenza virus ; Antivirals
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：15 January 2010
• 年：2010
• 卷：18
• 期：2
• 页码：839-848
• 全文大小：507 K

文摘

Chemotherapy and chemoprophylaxis of influenza is one of the most important directions of health protection activity. Due to the high rate of drug-resistant strains of influenza virus, there is a need for the search and further development of new potent antivirals against influenza with a broad spectrum of activity. In the present study, a set of di-, tri- and tetrazole derivatives of adamantane was efficiently prepared and their anti-influenza activities evaluated against rimantadine-resistant strain A/Puerto Rico/8/34. In general, derivatives of tetrazole possessed the highest virus-inhibiting activity. We demonstrated that several compounds of this set exhibited much higher activity than the currently used antiviral rimantadine, a compound of related structure. Moreover, we showed that these azolo-adamantanes were significantly less toxic. This study demonstrates that influenza viruses can be inhibited by adamantyl-azoles and thus have potential for developing antiviral agents with an alternate mechanism of action.