1. Academic Validation
  2. Synthesis and anti-viral activity of azolo-adamantanes against influenza A virus

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

  • Bioorg Med Chem. 2010 Jan 15;18(2):839-48. doi: 10.1016/j.bmc.2009.11.047.
Vladimir V Zarubaev 1 Efim L Golod Pavel M Anfimov Anna A Shtro Victor V Saraev Alexey S Gavrilov Alexander V Logvinov Oleg I Kiselev
Affiliations

Affiliation

  • 1 Department of Chemotherapy, Influenza Research Institute, 15/17 Prof. Popova St., 197376 St. Petersburg, Russia. zarubaev@influenza.spb.ru
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.

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