Центральная Научная Библиотека УрО РАН

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   T 44


    Лечебная эффективность нового отечественного химиопрепарата Триазавирин в отношении возбудителя гриппа А (H5N1) = Therapeutic efficacy of triazavirin, a novel russian chemotherapeutic, against influenza virus A (H5N1) / S. A. Loginova, S. V. Borisevich, V. A. Maksimov, V. P. Bondarev, S. K. Kotovskaya, V. L. Rusinov, V. N. Charushin, O. N. Chupakhin // Антибиотики и химиотерапия. - 2011. - Т. 56, № 1-2. - С. 10-12. - Библиогр.: с. 12 (13 назв.)

ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ТРИАЗАВИРИН -- ВИРУС ГРИППА A

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   A 62


    Antiviral Properties, Metabolism, and Pharmacokinetics of a Novel Azolo-1,2,4-Triazine-Derived Inhibitor of Influenza A and B Virus Replication [Text] / I. L. Karpenko, S. L. Deev, O. I. Kiselev, V. N. Charushin, V. L. Rusinov, E. N. Ulomskii, E. G. Deeva, O. N. Chupakhin // Antimicrobial Agents and Chemotherapy. - 2010. - Vol. 54, № 5. - P2017-2022

ББК 54
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

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   A 10


    A new antiviral drug triazavirin: Results of phase II clinical trial [Электронный ресурс] / O. I. Kiselev, E. G. Deyeva, T. I. Melnicova, K. N. Kozeletskaia, A. S. Klselev, V. L. Rusinov, V. N. Charushin, O. N. Chupakhin // Voprosy Virusologii . - 2012. - Vol.57, №6. - P9-12

ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
CLINICAL TRIAL -- EFFICACY -- INFLUENZA
Аннотация: The results of the clinical trial testing the efficacy of a new anti-influenza drug Triazavirin are presented in this work. The data of the trial were gathered during the 2010 influenza season. The treatment with oral Triazavirin significantly reduced the duration of the main clinical symptoms of influenza (intoxication, fever, respiratory symptoms), decreased the incidence of the influenza-related complications and the use of symptomatic drugs. The re-isolation rate of the influenza A and B viruses was significantly lower in the patients who were using Triazavirin. The analysis of the clinical data showed that the optimal prescribed dosage was 250 mg 3 times a day. -------------------------------------------------------------------------------- Reaxys Database Information|

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   T 86


    Triazaverin prophylactic efficacy against influenza virus A (H5N1) [Электронный ресурс] / S. Ya. Loginova, S. V. Borisevich, B. A. Maksimov, V. P. Bondarev, S. K. Kotovskaya, V. L. Rusinov, V. N. Charushin, O. N. Chupakhin // Antibiotiki i Khimioterapiya . - 2010. - Vol.55, №9-10. - P25-28

ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ANTIVIRAL EFFICACY -- INFLUENZA VIRUS A -- PROPHYLAXIS
Аннотация: The experimental study of the prophylactic efficacy of Triazaverin against the experimental form of the influenza virus A (H5N1) on albino mice intranasally infected with the influenza virus A/Chicken/Kurgan/Russia/02/05 vs. the reference drugs Tamiflu ®, Remantadin and Arbidol ® showed that in doses of 1 to 100 mg/kg it was efficient in the animal protection from death. The drug was also efficient in the urgent prophylaxis. Triazaverin effectively inhibited the influenza A virus multiplication in the lungs of the albino mice

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   A 62


    Antiviral properties, metabolism, and pharmacokinetics of a novel azolo-1,2,4-triazine-derived inhibitor of influenza A and B virus replication [Электронный ресурс] / I. L. Karpenko, S. L. Deev, O. I. Kiselev, V. N. Charushin, V. L. Rusinov, E. N. Ulomskii, E. G. Deeva, M. K. Kukhanova // Antimicrobial Agents and Chemotherapy . - 2010. - Vol.54, №5. - P2017-2022

ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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   I-70


    Investigation of triazavirin antiviral activity against influenza A virus (H5N1) in cell culture [Электронный ресурс] / S. Ya. Loginova, S. V. Borisevich, V. A. Maksimov, V. P. Bondarev, S. K. Kotovskaya, V. L. Rusinov, V. N. Charushin // Antibiotiki i Khimioterapiya . - 2007. - Vol.52, №11-12. - P18-20

ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ANTIVIRAL ACTIVITY -- ARBIDOL -- INFLUENZA
Аннотация: Analysis of triazavirin efficacy with respect to influenza A virus (H5N1) in sensitive cell culture MDSK vs. effective antigrippe drugs, such as tamiflu, remantadin and arbidol showed that triazavirin in a wide range of the concentrations was efficient in inhibition of the virus cytopathic activity and formation of the specific hemagglutinin

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   N 89


    Novel purine conjugates with N-heterocycles: synthesis and anti-influenza activity / V. P. Krasnov, V. V. Zarubaev, D. V. Gruzdev [et al.] // Chemistry of Heterocyclic Compounds. - 2021. - Vol. 57, № 4. - P498-504

УДК

Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
6-CHLOROPURINE -- HETEROCYCLIC AMINES -- ANTIVIRAL ACTIVITY -- INFLUENZA A AND B VIRUSES
Аннотация: A number of novel amides were synthesized by coupling of 6-[(9H-purin-6-yl)amino]hexanoic acid to heterocyclic amines. The antiviral activity of the obtained compounds, as well as of purine conjugates in which 7,8-difluoro-3-methyl-3,4-dihydro-2H-1,4-benzoxazine is linked to position 6 of purine through a fragment of ɷ-amino acids with varying lengths of polymethylene chains against influenza A and B viruses was studied in vitro. Purine derivatives have been shown to have moderate activity against influenza A (H1N1) virus. The antiinfluenza activity and cytotoxicity of conjugates with 7,8-difluoro-3-methyl-3,4-dihydro-2H-1,4-benzoxazine depend on the length of the linker fragment.

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    Synthesis of pyrimidine conjugates with 4-(6-amino-hexanoyl)-7,8-difluoro-3,4-dihydro-3-methyl-2h-[1,4] benzoxazine and evaluation of their antiviral activity / V. P. Krasnov, V. V. Musiyak, G. L. Levit [et al.] // Molecules. - 2022. - Vol. 27, № 13. - Ст. 4236
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRIMIDINE
Аннотация: A series of pyrimidine conjugates containing a fragment of racemic 7,8-difluoro-3,4-dihydro-3-methyl-2H-[1,4]benzoxazine and its (S)-enantiomer attached via a 6-aminohexanoyl fragment were synthesized by the reaction of nucleophilic substitution of chlorine in various chloropyrimidines. The structures of the synthesized compounds were confirmed by 1H, 19F, and 13C NMR spectral data. Enantiomeric purity of optically active derivatives was confirmed by chiral HPLC. Antiviral evaluation of the synthesized compounds has shown that the replacement of purine with a pyrimidine fragment leads to a decrease in the anti-herpesvirus activity compared to the lead compound, purine conjugate. The studied compounds did not exhibit significant activity against influenza A (H1N1) virus.

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