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.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ТРИАЗАВИРИН -- ВИРУС ГРИППА A |
T 80 Toxicity of Triazavirin, a Novel Russian Antiinfluenza chemotherapeutic [Электронный ресурс] / S. A. Loginova, S. V. Borisevich, V. L. Rusinov, E. N. Ulomskii, V. N. Charushin, O. N. Chupakhin> // Antibiotiki i Khimioterapiya . - 2012. - Vol.57, №11-12. - 8-10. Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): MICE -- TOXICITY -- TRIAZAVIRIN Аннотация: The study of the toxicity of triazavirin, a new antiinfluenza agent, showed that the maximum concentration of the drug, inducing no microscopically visible changes in the structure of the monolayer and the cells of the MDCK and SKEV cell cultures, was 128 and 100 mcg/ml respectively. The maximum drug dose for single intraperitoneal administration inducing no signs of acute intoxication in albino mice weighing 10-12 g was 1000 mg/kg. In investigation of the chronic toxicity it was shown that oral administration of the drug (by 0.05 ml) to the albino mice in a dose of 200 mg/kg (maximum possible concentration by the solubility) daily for 10 days was well tolerated by the laboratory animals. The maximum tolerable dose of triazavirin for the albino mice was >200 mg/kg. |
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 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| |
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 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 |
N 91 Nucleophilic substitution of nitro group in nitrotriazolotriazines as a model of potential interaction with cysteine-containing proteins [Electronic resource] / V. L. Rusinov, I. M. Sapozhnikova, E. N. Ulomskii, N. Medvedeva, V. V. Egorov, O. I. Kiselev, E. G. Deeva, A. V. Vasin, O. N. Chupakhin> // Chemistry of Heterocyclic Compounds. - 2015. - Vol. 51, № 3. - С. 275-280. - Bibliogr. : p. 280 (17 ref.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): AZOLO[5,1-C]TRIAZINES -- GLUTATHIONE -- CYSTEINE Аннотация: Azolo[5,1-c]triazines, cysteine, glutathione, nitro compounds, Triazavirin, metabolic transformations, nucleophilic substitution \\\\expert2\\nbo\\Chemistry of Heterocyclic Compounds\\2015, v.51, N 3, p. 275-280.pdf |
C 57 Chupakhin, O. N. Scientific foundations for the creation of antiviral and antibacterial preparations [Electronic resource] / O. N. Chupakhin, V. N. Charushin, V. L. Rusinov> // Herald of the Russian Academy of Sciences. - 2016. - Vol. 86, № 3. - С. 206-212 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): 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 |
A 62 Antiviral drug Triazavirin, selectively labeled with 2H, 13C, and 15N stable isotopes. Synthesis and properties / T. S. Shestakova, S. L. Deev, I. A. Khalymbadzha [et al.]> // Chemistry of Heterocyclic Compounds. - 2021. - Vol. 57, № 4. - P479–482
Кл.слова (ненормированные): ТРИАЗАВИРИН |
R 32 Redox conversions of new antiviral drug Triazavirin®: electrochemical study and esr spectroscopy / A. V. Ivoilova, A. N. Tsmokalyuk, A. N. Kozitsina [et al.]> // Russian chemical bulletin. - 2021. - Vol. 70, № 6. - P1099-1108 Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ Кл.слова (ненормированные): TRIAZAVIRIN -- ANTIVIRAL DRUGS -- REDOX CONVERSIONS -- CYCLIC VOLTAMMETRY -- ESR SPECTROSCOPY -- CHRONOAMPEROMETRY Аннотация: The results of studying electrochemical conversions of 7-R-3-X-1,2,4-triazolo[5,1-c][1,2,4]-triazin-4-ones (Triazavirin® and its derivatives) using cyclic voltammetry, chronoamperometry, and ESR spectroscopy are presented. The derivatives of 7-R-3-X-1,2,4-triazolo[5,1-c][1,2,4]-triazin-4-ones were found to be capable of electrochemical reducing in the potential range from −0.16 to −0.68 V (vs Ag/AgCl) in a Britton—Robinson buffer at pH 2–12. At the potentials of the first electroreduction step at pH 2–6, the main process of transformations is the four-electron scheme of reduction of the nitro group of Triazavirin®. The adduct of the radical substances with the spin probe N-(1-hydroxy-2,2,6,6-tetramethylpiperidin-4-yl)-2-methylpropanamide was registered after the preliminary generation of the Triazavirin® radical anion at −0.5 V vs Ag/AgCl in an acidic medium. A linear dependence of the current of the first electroreduction step of the Triazavirin® on the concentration was obtained at pH 2 (linearity range from 10−4 to 1.6 · 10−2 mol L−1, I = −1.93 · C, R2 = 0.9977). |
Detection of anti-viral drug riamilovir and herbicides in aqueous media by using pyrene-based fluorescent chemosensors / I. S. Kovalev, L. K. Sadieva, O. S. Taniya [et al.]> // Chimica Techno Acta. - 2021. - Vol. 8, № 2. - P20218208 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): COVID-19 -- RIAMILOVIR -- TRIAZAVIRIN -- DETECTION IN AQUEOUS MEDIA -- FLUORESCENCE QUENCHING Аннотация: Two ethyleneglycol esters of 1-pyrene carboxylic acid were studied as chemosensors for the fluorescence “turn-off” detection of two nitro-containing analytes, such as antiviral drug Riamilovir (Triazavirin ®) and herbicidal agent dinitro-ortho-cresol (DNOC). In both cases the dramatic fluorescence quenching was observed with quenching constants as high as 3·104 M-1 and limits of detection (LOD) as low as 100 ppb. |
Pyrene-based lipophilic/biphilic chemosensors for the fluorescence "turn-off" detection of nitroanalytes in aqueous media / I. S. Kovalev, L. K. Sadieva, O. S. Taniya [и др.]> // AIP Conference Proceedings. - 2021. - Vol. 2388, № 1. - Ст. 030015 Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: Two approaches towards “turn off” fluorescence detection of nitroanalytes (dinitro-ortho-cresol (DNOC), 2,4,6-trinitrotoluene (TNT) and Riamilovir (Triazavirin ®) are reported such as by tuning the chemosensors structure or by changing the environment. In both cases the great response was achieved with Stern-Volmer quenching constants (KSV) as high as 2.28–3.14 × 104 M−1 (for structure modification approach) and 4.67 × 105 M−1 (for changing of environment approach). |
Development of drugs with direct antiviral action based on azaheterocyclic systems / V. N. Charushin, V. L. Rusinov, M. V. Varaksin [et al.]> // Herald of the Russian academy of sciences. - 2022. - Vol. 92, № 4. - P505-510 Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ ХИМИЧЕСКИЕ НАУКИ Аннотация: This article discusses the results of studies carried out in recent years by a team of scientists from the Postovskii Institute of Organic Synthesis, Ural Branch, Russian Academy of Sciences, in cooperation with the First President of Russia Boris Yeltsin Ural Federal University, Ural State Medical University, Volgograd State Medical University, and other scientific and production organizations of the country to create triazavirin (riamilovir) and other direct etiotropic antiviral drugs based on azaheterocyclic derivatives. |