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1.

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., Chupakhin O. N.
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
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 IAK 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
\\\\expert2\\nbo\\Antimicrobal Agents and Chemotherapy\\2010. V. 54, N 5. P. 2017-2022.pdf
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2.

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
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3.

Вид документа : Статья из журнала
Шифр издания : 54/C 57
Автор(ы) : Chupakhin O. N., Charushin V. N., Rusinov V. L.
Заглавие : Scientific foundations for the creation of antiviral and antibacterial preparations [Электронный ресурс]
Место публикации : Herald of the Russian Academy of Sciences. - 2016. - Vol. 86, № 3. - С. 206-212
Систем. требования: http://download.springer.com/static/pdf/65/
Примечания : 26.10.16
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): triazide and azoloazine derivatives --triazavirin--protein disulfide isomerase
Аннотация: The results of the Ural scientific school's organic chemists on the creation of antiviral and antibacterial, including antitubercular, chemopreparations are considered. Basic research data were generalized on the synthesis and study of antiviral activity and the establishment of the metabolism and mechanism of azoloazine series compounds-azaanalogs of adenine and guanine, as well as their nucleosides, which led to the creation of a new family of antiviral substances. One of them, triazavirin, has become a regular therapeutic fixture as an antiflu preparation. The results of synthetic and biological studies on substituted pyrimidines, nucleosides of the benzimidazole and purine series, and other biologically active azaheterocycles are also discussed.
\\\\expert2\\NBO\\Herald of the Russian Academy of Sciences\\2016. V. 86, N 3. P. 206-212.pdf
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