Synthesis and anti-viral activity of azolo-adamantanes against influenza A virus |
| |
Authors: | Vladimir V Zarubaev Efim L Golod Pavel M Anfimov Anna A Shtro Victor V Saraev Alexey S Gavrilov Alexander V Logvinov Oleg I Kiselev |
| |
Institution: | 1. Department of Chemotherapy, Influenza Research Institute, 15/17 Prof. Popova St., 197376 St. Petersburg, Russia;2. Department of Organic Nitrogen Compounds, St. Petersburg State Institute of Technology, 26 Moskovsky Pr., 190013 St. Petersburg, Russia |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|