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Title: Synthesis and anti-viral activity of azolo-adamantanes against influenza A virus
Authors: Golod, Efim L
Anfimov, Pavel M
Shtro, Anna A
Saraev, Victor V
Gavrilov, Alexey S
Logvinov, Alexander V
Kiselev, Oleg I
Zarubaev, Vladimir V. 
Issue Date: 15-Jan-2010
Publisher: Elsevier
Journal: Bioorganic and Medicinal Chemistry 
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.
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2009.11.047
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