Вид документа : Статья из журнала Шифр издания : 54/A 62 Автор(ы) : Karpenko I. L., Deev S. L., Kiselev O. I., Charushin V. N., Rusinov V. L., Ulomskii E. N., Deeva E.G., Kukhanova M. K. Заглавие : Antiviral properties, metabolism, and pharmacokinetics of a novel azolo-1,2,4-triazine-derived inhibitor of influenza A and B virus replication Место публикации : Antimicrobial Agents and Chemotherapy . - 2010. - Vol.54, №5. - С. 2017-2022 ББК : 54 Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ Ключевые слова (''Своб.индексиров.''): animal cell--animal experiment--antiviral activity 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(4Í)-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(4Í)-one} was discovered inÍÅK 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 Доп.точки доступа: Karpenko, I. L.; Deev, S. L.; Kiselev, O. I.; Charushin, V. N.; Rusinov, V. L.; Ulomskii, E. N.; Deeva, E.G.; Kukhanova, M. K.