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Antiviral Properties, Metabolism, and Pharmacokinetics of a Novel Azolo-1,2,4-Triazine-Derived Inhibitor of Influenza A and B Virus Replicationстатья
Статья опубликована в высокорейтинговом журнале
Информация о цитировании статьи получена из
Web of Science,
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 11 декабря 2015 г.
- Авторы: Karpenko I., Deev S., Kiselev O., Charushin V., Rusinov V., Ulomsky E., Deeva E., Yanvarev D., Ivanov A., Smirnova O.
- Журнал: Antimicrobial Agents and Chemotherapy
- Том: 54
- Номер: 5
- Год издания: 2010
- Издательство: American Society for Microbiology
- Местоположение издательства: United States
- Первая страница: 2017
- Последняя страница: 2022
- DOI: 10.1128/aac.01186-09
- Аннотация: Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine {2-methylthio-6-nitro-1,2,4-triazolo[ 5,1-c]-1,2,4-triazine-7(4I)-one} (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV {2-methylthio-6-amino-1,2,4-triazolo[ 5,1-s]-1,2,4-triazin(e)-7(4I)-one} was discovered in I angstrom K 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination.
- Добавил в систему: Кочетков Сергей Николаевич